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75747-14-7

75747-14-7 | 17-AAG

CAS No: 75747-14-7 Catalog No: AG005IF5 MDL No:MFCD04973892

Product Description

Catalog Number:
AG005IF5
Chemical Name:
17-AAG
CAS Number:
75747-14-7
Molecular Formula:
C31H43N3O8
Molecular Weight:
585.6884
MDL Number:
MFCD04973892
IUPAC Name:
[(4E,6Z,8S,9S,10E,12S,13R,14S,16R)-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-19-(prop-2-enylamino)-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl] carbamate
InChI:
InChI=1S/C31H43N3O8/c1-8-12-33-26-21-13-17(2)14-25(41-7)27(36)19(4)15-20(5)29(42-31(32)39)24(40-6)11-9-10-18(3)30(38)34-22(28(21)37)16-23(26)35/h8-11,15-17,19,24-25,27,29,33,36H,1,12-14H2,2-7H3,(H2,32,39)(H,34,38)/b11-9-,18-10+,20-15+/t17-,19+,24+,25+,27-,29+/m1/s1
InChI Key:
AYUNIORJHRXIBJ-TXHRRWQRSA-N
SMILES:
C=CCNC1=C2C[C@@H](C)C[C@H](OC)[C@H](O)[C@@H](C)/C=C(\C)/[C@@H]([C@H](C=CC=C(C(=O)NC(=CC1=O)C2=O)C)OC)OC(=O)N
UNII:
4GY0AVT3L4
NSC Number:
330507

Properties

Complexity:
1210  
Compound Is Canonicalized:
Yes
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
6  
Defined Bond Stereocenter Count:
3  
Exact Mass:
585.305g/mol
Formal Charge:
0
Heavy Atom Count:
42  
Hydrogen Bond Acceptor Count:
9  
Hydrogen Bond Donor Count:
4  
Isotope Atom Count:
0
Molecular Weight:
585.698g/mol
Monoisotopic Mass:
585.305g/mol
Rotatable Bond Count:
7  
Topological Polar Surface Area:
166A^2
Undefined Atom Stereocenter Count:
0
Undefined Bond Stereocenter Count:
0
XLogP3:
2.6  

Literature

Title Journal
Exome sequencing of hepatocellular carcinomas identifies new mutational signatures and potential therapeutic targets. Nature genetics 20150501
Two novel ALK mutations mediate acquired resistance to the next-generation ALK inhibitor alectinib. Clinical cancer research : an official journal of the American Association for Cancer Research 20141115
Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors. European journal of medicinal chemistry 20141006
A phase I study of the HSP90 inhibitor retaspimycin hydrochloride (IPI-504) in patients with gastrointestinal stromal tumors or soft-tissue sarcomas. Clinical cancer research : an official journal of the American Association for Cancer Research 20131101
Molecular markers for novel therapeutic strategies in pancreatic endocrine tumors. Pancreas 20130401
Inhibition of rapamycin-induced Akt phosphorylation by cotylenin A correlates with their synergistic growth inhibition of cancer cells. International journal of oncology 20130201
Lapatinib and 17AAG reduce 89Zr-trastuzumab-F(ab')2 uptake in SKBR3 tumor xenografts. Molecular pharmaceutics 20121105
Increased expression of heat shock protein 90 under chemical hypoxic conditions protects cardiomyocytes against injury induced by serum and glucose deprivation. International journal of molecular medicine 20121101
Pharmacokinetic study of 3-in-1 poly(ethylene glycol)-block-poly(D, L-lactic acid) micelles carrying paclitaxel, 17-allylamino-17-demethoxygeldanamycin, and rapamycin. Journal of controlled release : official journal of the Controlled Release Society 20121010
HSP90 inhibition results in apoptosis of Philadelphia acute lymphoblastic leukaemia cells: an attractive prospect of new targeted agents. Journal of cancer research and clinical oncology 20121001
17-allylamino-17-(demethoxy)geldanamycin (17-AAG) is a potent and effective inhibitor of human cytomegalovirus replication in primary fibroblast cells. Archives of virology 20121001
Antitumor activity of Triolimus: a novel multidrug-loaded micelle containing Paclitaxel, Rapamycin, and 17-AAG. Molecular cancer therapeutics 20121001
Ganetespib (STA-9090), a nongeldanamycin HSP90 inhibitor, has potent antitumor activity in in vitro and in vivo models of non-small cell lung cancer. Clinical cancer research : an official journal of the American Association for Cancer Research 20120915
EC144 is a potent inhibitor of the heat shock protein 90. Journal of medicinal chemistry 20120913
Multiple kinase pathways involved in the different de novo sensitivity of pancreatic cancer cell lines to 17-AAG. The Journal of surgical research 20120701
17-Allylamino-17-demethoxygeldanamycin and ritonavir inhibit renal cancer growth by inhibiting the expression of heat shock factor-1. International journal of oncology 20120701
Inhibition of thymidine phosphorylase expression by using an HSP90 inhibitor potentiates the cytotoxic effect of cisplatin in non-small-cell lung cancer cells. Biochemical pharmacology 20120701
Isoxazolo(aza)naphthoquinones: a new class of cytotoxic Hsp90 inhibitors. European journal of medicinal chemistry 20120701
Evidence for efficacy of new Hsp90 inhibitors revealed by ex vivo culture of human prostate tumors. Clinical cancer research : an official journal of the American Association for Cancer Research 20120701
17-AAG mediated targeting of Hsp90 limits tert activity in peritoneal sarcoma related malignant ascites by downregulating cyclin D1 during cell cycle entry. Experimental oncology 20120701
Inhibition of the mTORC2 and chaperone pathways to treat leukemia. Blood 20120621
Hsp90 regulates O-linked β-N-acetylglucosamine transferase: a novel mechanism of modulation of protein O-linked β-N-acetylglucosamine modification in endothelial cells. American journal of physiology. Cell physiology 20120615
Blockade of XBP1 splicing by inhibition of IRE1α is a promising therapeutic option in multiple myeloma. Blood 20120614
Constitutive AhR activation leads to concomitant ABCG2-mediated multidrug resistance in cisplatin-resistant esophageal carcinoma cells. Molecular carcinogenesis 20120601
Expression and therapeutic relevance of heat-shock protein 90 in pancreatic endocrine tumors. Endocrine-related cancer 20120601
Folate receptor targeted 17-allylamino-17-demethoxygeldanamycin (17-AAG) loaded polymeric nanoparticles for breast cancer. Colloids and surfaces. B, Biointerfaces 20120601
Novel molecular targeted therapies for refractory thyroid cancer. Head & neck 20120501
Clinical experience with the heat shock protein-90 inhibitor, tanespimycin, in patients with relapsed lymphoma. Leukemia & lymphoma 20120501
Heat shock protein 90 is a promising target for effective growth inhibition of gastrointestinal neuroendocrine tumors. International journal of oncology 20120501
Fluorescent protein-labeled glucocorticoid receptor alpha isoform trafficking in cultured human trabecular meshwork cells. Investigative ophthalmology & visual science 20120501
Hsp90 interacts specifically with viral RNA and differentially regulates replication initiation of Bamboo mosaic virus and associated satellite RNA. PLoS pathogens 20120501
Hsp90 inhibitors and drug resistance in cancer: the potential benefits of combination therapies of Hsp90 inhibitors and other anti-cancer drugs. Biochemical pharmacology 20120415
NAD(P)H:quinone oxidoreductase 1 (NQO1) in the sensitivity and resistance to antitumor quinones. Biochemical pharmacology 20120415
A phase I trial of docetaxel and pulse-dose 17-allylamino-17-demethoxygeldanamycin in adult patients with solid tumors. Cancer chemotherapy and pharmacology 20120401
SUMO-2/3 conjugates accumulating under heat shock or MG132 treatment result largely from new protein synthesis. Biochimica et biophysica acta 20120401
Heat shock proteins as key biological targets of the marine natural cyclopeptide perthamide C. Molecular bioSystems 20120401
Protein kinase CK2 protects multiple myeloma cells from ER stress-induced apoptosis and from the cytotoxic effect of HSP90 inhibition through regulation of the unfolded protein response. Clinical cancer research : an official journal of the American Association for Cancer Research 20120401
Inhibition of p38 MAPK-dependent excision repair cross-complementing 1 expression decreases the DNA repair capacity to sensitize lung cancer cells to etoposide. Molecular cancer therapeutics 20120301
Identification of HSP90 as a new GABARAPL1 (GEC1)-interacting protein. Biochimie 20120301
Tipifarnib and tanespimycin show synergic proapoptotic activity in U937 cells. Journal of cancer research and clinical oncology 20120301
A Phase II trial of 17-allylamino, 17-demethoxygeldanamycin (17-AAG, tanespimycin) in patients with metastatic melanoma. Investigational new drugs 20120201
A phase II study of gemcitabine in combination with tanespimycin in advanced epithelial ovarian and primary peritoneal carcinoma. Gynecologic oncology 20120201
A phase II study of 17-allylamino-17-demethoxygeldanamycin in metastatic or locally advanced, unresectable breast cancer. Breast cancer research and treatment 20120201
Hsp90 inhibitors sensitise human colon cancer cells to topoisomerase I poisons by depletion of key anti-apoptotic and cell cycle checkpoint proteins. Biochemical pharmacology 20120201
Ganetespib, a unique triazolone-containing Hsp90 inhibitor, exhibits potent antitumor activity and a superior safety profile for cancer therapy. Molecular cancer therapeutics 20120201
Simultaneous inhibition of glutathione- and thioredoxin-dependent metabolism is necessary to potentiate 17AAG-induced cancer cell killing via oxidative stress. Free radical biology & medicine 20120115
In vitro assessment of cytochrome P450 inhibition and induction potential of tanespimycin and its major metabolite, 17-amino-17-demethoxygeldanamycin. Cancer chemotherapy and pharmacology 20120101
Cooperative enhancement of radiosensitivity after combined treatment of 17-(allylamino)-17-demethoxygeldanamycin and celecoxib in human lung and colon cancer cell lines. DNA and cell biology 20120101
In vitro drug treatments reduce the deleterious effects of aggregates containing polyAla expanded PHOX2B proteins. Neurobiology of disease 20120101
Cellular growth kinetics distinguish a cyclophilin inhibitor from an HSP90 inhibitor as a selective inhibitor of hepatitis C virus. PloS one 20120101
The aggregation and neurotoxicity of TDP-43 and its ALS-associated 25 kDa fragment are differentially affected by molecular chaperones in Drosophila. PloS one 20120101
Advances in establishment and analysis of three-dimensional tumor spheroid-based functional assays for target validation and drug evaluation. BMC biology 20120101
Effects of HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin (17-AAG) on NEU/HER2 overexpressing mammary tumours in MMTV-NEU-NT mice monitored by Magnetic Resonance Spectroscopy. BMC research notes 20120101
The effects of heat shock protein 90 inhibitors on apoptosis and viral replication in primary effusion lymphoma cells. Biological & pharmaceutical bulletin 20120101
Effects of Hsp90 inhibitors, geldanamycin and its analog, on ceramide metabolism and cytotoxicity in PC12 cells. The Journal of toxicological sciences 20120101
The role of hypoxia inducible factor-1α in the increased MMP-2 and MMP-9 production by human monocytes exposed to nickel nanoparticles. Nanotoxicology 20111201
Pharmacological inhibition of HSP90 activity negatively modulates myogenic differentiation and cell survival in C2C12 cells. Molecular and cellular biochemistry 20111201
Clusterin is a critical downstream mediator of stress-induced YB-1 transactivation in prostate cancer. Molecular cancer research : MCR 20111201
Inhibition of RPE cell sterile inflammatory responses and endotoxin-induced uveitis by a cell-impermeable HSP90 inhibitor. Experimental eye research 20111201
Synthesis and evaluation of poly(styrene-co-maleic acid) micellar nanocarriers for the delivery of tanespimycin. International journal of pharmaceutics 20111125
Phase I and pharmacological study of cytarabine and tanespimycin in relapsed and refractory acute leukemia. Haematologica 20111101
ATP analog enhances the actions of a heat shock protein 90 inhibitor in multiple myeloma cells. The Journal of pharmacology and experimental therapeutics 20111101
Identifying inhibitors of epithelial-mesenchymal transition by connectivity map-based systems approach. Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20111101
Multi-drug delivery to tumor cells via micellar nanocarriers. International journal of pharmaceutics 20111031
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The heat shock protein 90 inhibitor IPI-504 induces KIT degradation, tumor shrinkage, and cell proliferation arrest in xenograft models of gastrointestinal stromal tumors. Molecular cancer therapeutics 20111001
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Exploiting cancer cell vulnerabilities to develop a combination therapy for ras-driven tumors. Cancer cell 20110913
Novel insights into the role of HSP90 in cytoprotection of H2S against chemical hypoxia-induced injury in H9c2 cardiac myocytes. International journal of molecular medicine 20110901
Heat shock protein 90 inhibition results in altered downstream signaling of mutant KIT and exerts synergistic effects on Kasumi-1 cells when combining with histone deacetylase inhibitor. Leukemia research 20110901
Clusterin inhibition using OGX-011 synergistically enhances Hsp90 inhibitor activity by suppressing the heat shock response in castrate-resistant prostate cancer. Cancer research 20110901
The Novel HSP90 inhibitor, IPI-493, is highly effective in human gastrostrointestinal stromal tumor xenografts carrying heterogeneous KIT mutations. Clinical cancer research : an official journal of the American Association for Cancer Research 20110901
Synthesis and evaluation of biotinylated sansalvamide A analogs and their modulation of Hsp90. Bioorganic & medicinal chemistry letters 20110815
HSP90 inhibition is effective in breast cancer: a phase II trial of tanespimycin (17-AAG) plus trastuzumab in patients with HER2-positive metastatic breast cancer progressing on trastuzumab. Clinical cancer research : an official journal of the American Association for Cancer Research 20110801
A 3-in-1 polymeric micelle nanocontainer for poorly water-soluble drugs. Molecular pharmaceutics 20110801
Why is this effective HSP90 inhibitor not being developed in HER2+ breast cancer? Clinical cancer research : an official journal of the American Association for Cancer Research 20110801
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Impaired infectivity of ritonavir-resistant HIV is rescued by heat shock protein 90AB1. The Journal of biological chemistry 20110715
HSP70 inhibition by the small-molecule 2-phenylethynesulfonamide impairs protein clearance pathways in tumor cells. Molecular cancer research : MCR 20110701
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Determination of the volume changes induced by ligand binding to heat shock protein 90 using high-pressure denaturation. Analytical biochemistry 20110615
Fibroblast growth factor receptor 3 (FGFR3) is a strong heat shock protein 90 (Hsp90) client: implications for therapeutic manipulation. The Journal of biological chemistry 20110603
The Hsp90 inhibitor IPI-504 rapidly lowers EML4-ALK levels and induces tumor regression in ALK-driven NSCLC models. Oncogene 20110602
Phase I study of 17-allylamino-17 demethoxygeldanamycin, gemcitabine and/or cisplatin in patients with refractory solid tumors. Investigational new drugs 20110601
Hsp90 regulates NADPH oxidase activity and is necessary for superoxide but not hydrogen peroxide production. Antioxidants & redox signaling 20110601
Tanespimycin and bortezomib combination treatment in patients with relapsed or relapsed and refractory multiple myeloma: results of a phase 1/2 study. British journal of haematology 20110601
Tanespimycin pharmacokinetics: a randomized dose-escalation crossover phase 1 study of two formulations. Cancer chemotherapy and pharmacology 20110501
Protection of murine neural progenitor cells by the Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin in the low nanomolar concentration range. Journal of neurochemistry 20110501
Blockade of Hsp90 by 17AAG antagonizes MDMX and synergizes with Nutlin to induce p53-mediated apoptosis in solid tumors. Cell death & disease 20110501
[Effect of heat shock protein 90 inhibitor 17-dimethylamino-ethylaminogeldanamycin on TNfalpha-mediated apoptosis and TNF-induced NF-kappaB activation]. Sichuan da xue xue bao. Yi xue ban = Journal of Sichuan University. Medical science edition 20110501
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Role for NAD(P)H:quinone oxidoreductase 1 and manganese-dependent superoxide dismutase in 17-(allylamino)-17-demethoxygeldanamycin-induced heat shock protein 90 inhibition in pancreatic cancer cells. The Journal of pharmacology and experimental therapeutics 20110301
HSP90 is crucial for regulation of LAT expression in activated T cells. Molecular immunology 20110301
Identification of aneuploidy-selective antiproliferation compounds. Cell 20110218
Carbamazepine promotes Her-2 protein degradation in breast cancer cells by modulating HDAC6 activity and acetylation of Hsp90. Molecular and cellular biochemistry 20110201
Inhibition of heat shock protein 90 (HSP90) as a therapeutic strategy for the treatment of myeloma and other cancers. British journal of haematology 20110201
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The role of heat shock protein 90 in the regulation of tumor cell apoptosis. Bulletin of experimental biology and medicine 20110201
The Hsp90 inhibitor IPI-504 overcomes bortezomib resistance in mantle cell lymphoma in vitro and in vivo by down-regulation of the prosurvival ER chaperone BiP/Grp78. Blood 20110127
17-AAG increases autophagic removal of mutant androgen receptor in spinal and bulbar muscular atrophy. Neurobiology of disease 20110101
Mechanisms by which interleukin-6 regulates prostate-specific antigen gene expression in prostate LNCaP carcinoma cells. Journal of andrology 20110101
Targeted inhibition of multiple receptor tyrosine kinases in mesothelioma. Neoplasia (New York, N.Y.) 20110101
Expression-based in silico screening of candidate therapeutic compounds for lung adenocarcinoma. PloS one 20110101
High-content, high-throughput analysis of cell cycle perturbations induced by the HSP90 inhibitor XL888. PloS one 20110101
Cytotoxicity testing: measuring viable cells, dead cells, and detecting mechanism of cell death. Methods in molecular biology (Clifton, N.J.) 20110101
SNX-2112, a novel Hsp90 inhibitor, induces G2/M cell cycle arrest and apoptosis in MCF-7 cells. Bioscience, biotechnology, and biochemistry 20110101
Sulforaphane potentiates the efficacy of 17-allylamino 17-demethoxygeldanamycin against pancreatic cancer through enhanced abrogation of Hsp90 chaperone function. Nutrition and cancer 20110101
[Heat shock protein 90--modulator of TNFalpha-induced apoptosis of Jurkat tumor cells]. Vestnik Rossiiskoi akademii meditsinskikh nauk 20110101
Targeting HSP90 in ovarian cancers with multiple receptor tyrosine kinase coactivation. Molecular cancer 20110101
Magnetic resonance spectroscopy detectable metabolomic fingerprint of response to antineoplastic treatment. PloS one 20110101
Assessment of hypoxia inducible factor levels in cancer cell lines upon hypoxic induction using a novel reporter construct. PloS one 20110101
Hsp90 (heat shock protein 90) inhibitor occupancy is a direct determinant of client protein degradation and tumor growth arrest in vivo. The Journal of biological chemistry 20101217
N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors. Bioorganic & medicinal chemistry letters 20101215
Mineralocorticoid receptor degradation is promoted by Hsp90 inhibition and the ubiquitin-protein ligase CHIP. American journal of physiology. Renal physiology 20101201
Assaying pharmacodynamic endpoints with targeted therapy: flavopiridol and 17AAG induced dephosphorylation of histone H1.5 in acute myeloid leukemia. Proteomics 20101201
Heat shock protein 90 regulates the expression of Wilms tumor 1 protein in myeloid leukemias. Blood 20101125
Activity of IPI-504, a novel heat-shock protein 90 inhibitor, in patients with molecularly defined non-small-cell lung cancer. Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20101120
Prevention of autosomal dominant retinitis pigmentosa by systemic drug therapy targeting heat shock protein 90 (Hsp90). Human molecular genetics 20101115
Schwann cell autophagy induced by SAHA, 17-AAG, or clonazepam can reduce bortezomib-induced peripheral neuropathy. British journal of cancer 20101109
Identification of a novel HSP70-binding cochaperone critical to HSP90-mediated activation of small serine/threonine kinase. The Journal of biological chemistry 20101105
Heat shock protein 90 inhibition depletes LATS1 and LATS2, two regulators of the mammalian hippo tumor suppressor pathway. Cancer research 20101101
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. Bioorganic & medicinal chemistry letters 20101101
Targeting heat shock protein 72 enhances Hsp90 inhibitor-induced apoptosis in myeloma. Leukemia 20101001
The novel Hsp-90 inhibitor SNX7081 is significantly more potent than 17-AAG against primary CLL cells and a range of haematological cell lines, irrespective of lesions in the TP53 pathway. British journal of haematology 20101001
Protection of oligodendrocyte precursor cells by low doses of HSP90 inhibitors in cell culture. Experimental neurology 20100901
Molecular markers for novel therapies in neuroendocrine (carcinoid) tumors. Endocrine-related cancer 20100901
Inhibition of heat-shock protein 90 reduces Ebola virus replication. Antiviral research 20100801
Geldanamycin and its analog induce cytotoxicity in cultured human retinal pigment epithelial cells. Experimental eye research 20100801
Tanespimycin monotherapy in relapsed multiple myeloma: results of a phase 1 dose-escalation study. British journal of haematology 20100801
Tanespimycin with bortezomib: activity in relapsed/refractory patients with multiple myeloma. British journal of haematology 20100801
Safety, efficacy, pharmacokinetics, and pharmacodynamics of the combination of sorafenib and tanespimycin. Clinical cancer research : an official journal of the American Association for Cancer Research 20100715
RET is a heat shock protein 90 (HSP90) client protein and is knocked down upon HSP90 pharmacological block. The Journal of clinical endocrinology and metabolism 20100701
Modulation of melanoma cell phospholipid metabolism in response to heat shock protein 90 inhibition. Oncotarget 20100701
Phosphatidylcholine metabolic transformation and progression signature as a pharmacodynamic biomarker. Oncotarget 20100701
A simple yeast-based system for analyzing inhibitor resistance in the human cancer drug targets Hsp90alpha/beta. Biochemical pharmacology 20100601
Reactive oxygen species mediate hepatotoxicity induced by the Hsp90 inhibitor geldanamycin and its analogs. Free radical biology & medicine 20100601
HSP90 inhibitors induce desensitization of EGF receptor via p38 MAPK-mediated phosphorylation at Ser1046/1047 in human pancreatic cancer cells. Oncology reports 20100601
Heat shock protein 90 inhibitors attenuate inflammatory responses in atherosclerosis. Cardiovascular research 20100501
Hsp90 inhibitors: a potential treatment for latent EBV infection? Cell cycle (Georgetown, Tex.) 20100501
17-allylamino-17-demethoxygeldanamycin and MEK1/2 inhibitors kill GI tumor cells via Ca2+-dependent suppression of GRP78/BiP and induction of ceramide and reactive oxygen species. Molecular cancer therapeutics 20100501
Specific regulation of noncanonical p38alpha activation by Hsp90-Cdc37 chaperone complex in cardiomyocyte. Circulation research 20100430
Hsp90 directly modulates the spatial distribution of AF9/MLLT3 and affects target gene expression. The Journal of biological chemistry 20100416
Targeting the 90 kDa heat shock protein improves photodynamic therapy. Cancer letters 20100328
Combination therapy for hepatitis C virus with heat-shock protein 90 inhibitor 17-AAG and proteasome inhibitor MG132. Antiviral chemistry & chemotherapy 20100309
17-AAG, a Hsp90 inhibitor, attenuates the hypoxia-induced expression of SDF-1alpha and ILK in mouse RPE cells. Molecular biology reports 20100301
BIIB021, a novel Hsp90 inhibitor, sensitizes head and neck squamous cell carcinoma to radiotherapy. International journal of cancer 20100301
BIIB021, a synthetic Hsp90 inhibitor, has broad application against tumors with acquired multidrug resistance. International journal of cancer 20100301
[Management of metastatic HER2-positive breast cancer: present and future]. Bulletin du cancer 20100301
Hsp90-functionalized polypyrrole nanotube FET sensor for anti-cancer agent detection. Biosensors & bioelectronics 20100215
Heat shock protein 90: inhibitors in clinical trials. Journal of medicinal chemistry 20100114
The Hsp90 cochaperone, FKBP51, increases Tau stability and polymerizes microtubules. The Journal of neuroscience : the official journal of the Society for Neuroscience 20100113
Inhibition of 90-kD heat shock protein potentiates the cytotoxicity of chemotherapeutic agents in human glioma cells. Journal of neurosurgery 20100101
17-AAG induces cytoplasmic alpha-synuclein aggregate clearance by induction of autophagy. PloS one 20100101
Targeting Hsp90 with small molecule inhibitors induces the over-expression of the anti-apoptotic molecule, survivin, in human A549, HONE-1 and HT-29 cancer cells. Molecular cancer 20100101
Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin inhibits the proliferation of ARPE-19 cells. Journal of biomedical science 20100101
Bcl-2 regulates HIF-1alpha protein stabilization in hypoxic melanoma cells via the molecular chaperone HSP90. PloS one 20100101
17-Allylamino-17-demethoxygeldanamycin induces downregulation of critical Hsp90 protein clients and results in cell cycle arrest and apoptosis of human urinary bladder cancer cells. BMC cancer 20100101
Molecular signature of response and potential pathways related to resistance to the HSP90 inhibitor, 17AAG, in breast cancer. BMC medical genomics 20100101
17-allyamino-17-demethoxygeldanamycin treatment results in a magnetic resonance spectroscopy-detectable elevation in choline-containing metabolites associated with increased expression of choline transporter SLC44A1 and phospholipase A2. Breast cancer research : BCR 20100101
The antiproliferative activity of the heat shock protein 90 inhibitor IPI-504 is not dependent on NAD(P)H:quinone oxidoreductase 1 activity in vivo. Molecular cancer therapeutics 20091201
Induction of E-cadherin in lung cancer and interaction with growth suppression by histone deacetylase inhibition. Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20091201
Inhibition of constitutive and cxc-chemokine-induced NF-kappaB activity potentiates ansamycin-based HSP90-inhibitor cytotoxicity in castrate-resistant prostate cancer cells. British journal of cancer 20091103
Proton MRS detects metabolic changes in hormone sensitive and resistant human prostate cancer models CWR22 and CWR22r. Magnetic resonance in medicine 20091101
[Molecular therapy targeting protein misfolding and aggregation for the polyglutamine diseases]. Rinsho shinkeigaku = Clinical neurology 20091101
Anti-proliferative activity of heat shock protein (Hsp) 90 inhibitors via beta-catenin/TCF7L2 pathway in adult T cell leukemia cells. Cancer letters 20091018
Heat shock protein-90 inhibitors increase MHC class I-related chain A and B ligand expression on multiple myeloma cells and their ability to trigger NK cell degranulation. Journal of immunology (Baltimore, Md. : 1950) 20091001
Retaspimycin hydrochloride (IPI-504): a novel heat shock protein inhibitor as an anticancer agent. Expert opinion on investigational drugs 20090901
Met amplification and HSP90 inhibitors. Cell cycle (Georgetown, Tex.) 20090901
Candidate therapeutic agents for hepatocellular cancer can be identified from phenotype-associated gene expression signatures. Cancer 20090815
Enhanced radiosensitization of human glioma cells by combining inhibition of poly(ADP-ribose) polymerase with inhibition of heat shock protein 90. Molecular cancer therapeutics 20090801
Antitumor efficacy of IPI-504, a selective heat shock protein 90 inhibitor against human epidermal growth factor receptor 2-positive human xenograft models as a single agent and in combination with trastuzumab or lapatinib. Molecular cancer therapeutics 20090801
Three-kinase inhibitor combination recreates multipathway effects of a geldanamycin analogue on hepatocellular carcinoma cell death. Molecular cancer therapeutics 20090801
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. Journal of medicinal chemistry 20090723
Hsp90 inhibitors, GA and 17AAG, lead to ER stress-induced apoptosis in rat histiocytoma. Biochemical pharmacology 20090715
Zebularine suppresses the apoptotic potential of 5-fluorouracil via cAMP/PKA/CREB pathway against human oral squamous cell carcinoma cells. Cancer chemotherapy and pharmacology 20090701
Heat shock protein 90 inhibitor induces apoptosis and attenuates activation of hepatic stellate cells. The Journal of pharmacology and experimental therapeutics 20090701
Cancer cells harboring MET gene amplification activate alternative signaling pathways to escape MET inhibition but remain sensitive to Hsp90 inhibitors. Cell cycle (Georgetown, Tex.) 20090701
Potent triazolothione inhibitor of heat-shock protein-90. Chemical biology & drug design 20090701
Tanespimycin: the opportunities and challenges of targeting heat shock protein 90. Expert opinion on investigational drugs 20090601
Heat-shock protein 90 (Hsp90) as a molecular target for therapy of gastrointestinal cancer. Anticancer research 20090601
Potent cytotoxic C-11 modified geldanamycin analogues. Journal of medicinal chemistry 20090528
Transcription inhibition of heat shock proteins: a strategy for combination of 17-allylamino-17-demethoxygeldanamycin and actinomycin d. Cancer research 20090501
Integration of ligand and structure-based virtual screening for the identification of the first dual targeting agent for heat shock protein 90 (Hsp90) and tubulin. Journal of medicinal chemistry 20090423
Gene expression patterns in mismatch repair-deficient colorectal cancers highlight the potential therapeutic role of inhibitors of the phosphatidylinositol 3-kinase-AKT-mammalian target of rapamycin pathway. Clinical cancer research : an official journal of the American Association for Cancer Research 20090415
Efficacy of the HSP90 inhibitor 17-AAG in human glioma cell lines and tumorigenic glioma stem cells. Neuro-oncology 20090401
A cremophor-free formulation for tanespimycin (17-AAG) using PEO-b-PDLLA micelles: characterization and pharmacokinetics in rats. Journal of pharmaceutical sciences 20090401
High cytotoxic sensitivity of the oligodendrocyte precursor cells to HSP90 inhibitors in cell cultures. Experimental neurology 20090401
Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. Journal of medicinal chemistry 20090326
Discovery and development of heat shock protein 90 inhibitors. Bioorganic & medicinal chemistry 20090315
Acquired resistance to 17-allylamino-17-demethoxygeldanamycin (17-AAG, tanespimycin) in glioblastoma cells. Cancer research 20090301
The heat shock protein 90 inhibitor IPI-504 induces apoptosis of AKT-dependent diffuse large B-cell lymphomas. British journal of haematology 20090201
Targeted therapy of human osteosarcoma with 17AAG or rapamycin: characterization of induced apoptosis and inhibition of mTOR and Akt/MAPK/Wnt pathways. International journal of oncology 20090201
An experimental study on the antitumor effect of 131I-17-AAG in vitro and in vivo. Annals of nuclear medicine 20090201
Hsp90 is expressed and represents a therapeutic target in human oesophageal cancer using the inhibitor 17-allylamino-17-demethoxygeldanamycin. British journal of cancer 20090127
VIP-grafted sterically stabilized phospholipid nanomicellar 17-allylamino-17-demethoxy geldanamycin: a novel targeted nanomedicine for breast cancer. International journal of pharmaceutics 20090105
90-kDa heat shock protein inhibition abrogates the topoisomerase I poison-induced G2/M checkpoint in p53-null tumor cells by depleting Chk1 and Wee1. Molecular pharmacology 20090101
Effectiveness of 17DMAG, a geldanamycin derivative, in murine acute myeloid leukemia. Acta haematologica 20090101
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Inhibition and function of heat shock proteins 70 and 90. Current topics in medicinal chemistry 20090101
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Inhibition of telomerase activity by geldanamycin and 17-allylamino, 17-demethoxygeldanamycin in human melanoma cells. Carcinogenesis 20030501
ErbB2 degradation mediated by the co-chaperone protein CHIP. The Journal of biological chemistry 20030418
17AAG: low target binding affinity and potent cell activity--finding an explanation. Molecular cancer therapeutics 20030201
Auditing the pharmacological accounts for Hsp90 molecular chaperone inhibitors: unfolding the relationship between pharmacokinetics and pharmacodynamics. Molecular cancer therapeutics 20030201
Yeast is selectively hypersensitised to heat shock protein 90 (Hsp90)-targetting drugs with heterologous expression of the human Hsp90beta, a property that can be exploited in screens for new Hsp90 chaperone inhibitors. Gene 20030102
[Molecular chaperone HSP90 as a novel target for cancer chemotherapy]. Nihon yakurigaku zasshi. Folia pharmacologica Japonica 20030101
The role of functional and molecular imaging in cancer drug discovery and development. The British journal of radiology 20030101
Synthetic lethality: killing cancer with cancer. Journal of the National Cancer Institute 20021120
Challenges of PK/PD measurements in modern drug development. European journal of cancer (Oxford, England : 1990) 20021101
Molecular characterization and sensitivity of STI-571 (imatinib mesylate, Gleevec)-resistant, Bcr-Abl-positive, human acute leukemia cells to SRC kinase inhibitor PD180970 and 17-allylamino-17-demethoxygeldanamycin. Cancer research 20021015
Heat shock protein and proteasome targeting agents. Hematology/oncology clinics of North America 20021001
Heat shock protein inhibitor shows antitumor activity. Journal of the National Cancer Institute 20020821
Degradation of HER2 by ansamycins induces growth arrest and apoptosis in cells with HER2 overexpression via a HER3, phosphatidylinositol 3'-kinase-AKT-dependent pathway. Cancer research 20020601
Heat shock protein 90 inhibition by 17-allylamino-17- demethoxygeldanamycin: a novel therapeutic approach for treating hormone-refractory prostate cancer. Clinical cancer research : an official journal of the American Association for Cancer Research 20020501
17-Allylamino-17-demethoxygeldanamycin induces the degradation of androgen receptor and HER-2/neu and inhibits the growth of prostate cancer xenografts. Clinical cancer research : an official journal of the American Association for Cancer Research 20020501
Nucleophosmin-anaplastic lymphoma kinase (NPM-ALK), a novel Hsp90-client tyrosine kinase: down-regulation of NPM-ALK expression and tyrosine phosphorylation in ALK(+) CD30(+) lymphoma cells by the Hsp90 antagonist 17-allylamino,17-demethoxygeldanamycin. Cancer research 20020301
Suppressive effects of ansamycins on inducible nitric oxide synthase expression and the development of experimental autoimmune encephalomyelitis. Journal of neuroscience research 20020215
Ansamycin antibiotics inhibit Akt activation and cyclin D expression in breast cancer cells that overexpress HER2. Oncogene 20020214
HSP90 as a new therapeutic target for cancer therapy: the story unfolds. Expert opinion on biological therapy 20020101
Combining cytotoxics and 17-allylamino, 17-demethoxygeldanamycin: sequence and tumor biology matters. Commentary re: P. Münster et al., Modulation of Hsp90 function by ansamycins sensitizes breast cancer cells to chemotherapy-induced apoptosis in an RB- and schedule-dependent manner. Clin. Cancer Res., 7: 2228-2236, 2001. Clinical cancer research : an official journal of the American Association for Cancer Research 20010801
Modulation of Hsp90 function by ansamycins sensitizes breast cancer cells to chemotherapy-induced apoptosis in an RB- and schedule-dependent manner. See: E. A. Sausville, Combining cytotoxics and 17-allylamino, 17-demethoxygeldanamycin: sequence and tumor biology matters, Clin. Cancer Res., 7: 2155-2158, 2001. Clinical cancer research : an official journal of the American Association for Cancer Research 20010801
Inhibition of signal transduction by the Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin results in cytostasis and apoptosis. Cancer research 20010515
Disruption of the EF-2 kinase/Hsp90 protein complex: a possible mechanism to inhibit glioblastoma by geldanamycin. Cancer research 20010515
Measurement of the novel antitumor agent 17-(allylamino)-17-demethoxygeldanamycin in human plasma by high-performance liquid chromatography. Journal of chromatography. B, Biomedical sciences and applications 20010505
LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family. Bioorganic & medicinal chemistry letters 20010409
Inhibition of heat shock protein 90 function by ansamycins causes the morphological and functional differentiation of breast cancer cells. Cancer research 20010401
Plasma pharmacokinetics and tissue distribution of 17-(allylamino)-17-demethoxygeldanamycin (NSC 330507) in CD2F1 mice1. Cancer chemotherapy and pharmacology 20010401
Magnetic resonance detects changes in phosphocholine associated with Ras activation and inhibition in NIH 3T3 cells. British journal of cancer 20010301
Geldanamycin and its analogue 17-allylamino-17-demethoxygeldanamycin lowers Bcr-Abl levels and induces apoptosis and differentiation of Bcr-Abl-positive human leukemic blasts. Cancer research 20010301

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