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121569-61-7

121569-61-7 | 9,13-Epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-1-one, 2,3,10,11,12,13-hexahydro-3-hydroxy-10-methoxy-9-methyl-11-(methylamino)-, (3S,9S,10R,11R,13R)-

CAS No: 121569-61-7 Catalog No: AG0015A6 MDL No:

Product Description

Catalog Number:
AG0015A6
Chemical Name:
9,13-Epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-1-one, 2,3,10,11,12,13-hexahydro-3-hydroxy-10-methoxy-9-methyl-11-(methylamino)-, (3S,9S,10R,11R,13R)-
CAS Number:
121569-61-7
Molecular Formula:
C28H26N4O4
Molecular Weight:
482.5304
IUPAC Name:
18-hydroxy-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one
InChI:
InChI=1S/C28H26N4O4/c1-28-25(35-3)15(29-2)12-18(36-28)31-16-10-6-4-8-13(16)19-21-22(27(34)30-26(21)33)20-14-9-5-7-11-17(14)32(28)24(20)23(19)31/h4-11,15,18,25,27,29,34H,12H2,1-3H3,(H,30,33)
InChI Key:
PBCZSGKMGDDXIJ-UHFFFAOYSA-N
SMILES:
CNC1CC2OC(C1OC)(C)n1c3ccccc3c3c1c1n2c2ccccc2c1c1c3C(NC1=O)O

Properties

Complexity:
935  
Compound Is Canonicalized:
Yes
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
0
Defined Bond Stereocenter Count:
0
Exact Mass:
482.195g/mol
Formal Charge:
0
Heavy Atom Count:
36  
Hydrogen Bond Acceptor Count:
5  
Hydrogen Bond Donor Count:
3  
Isotope Atom Count:
0
Molecular Weight:
482.54g/mol
Monoisotopic Mass:
482.195g/mol
Rotatable Bond Count:
2  
Topological Polar Surface Area:
89.7A^2
Undefined Atom Stereocenter Count:
5  
Undefined Bond Stereocenter Count:
0
XLogP3:
2.7  

Literature

Title Journal
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Celecoxib enhances the radiosensitizing effect of 7-hydroxystaurosporine (UCN-01) in human lung cancer cell lines. International journal of radiation oncology, biology, physics 20120701
Inhibition of Eg5 acts synergistically with checkpoint abrogation in promoting mitotic catastrophe. Molecular cancer research : MCR 20120501
Chk'ing p53-deficient breast cancers. The Journal of clinical investigation 20120402
Targeting Chk1 in p53-deficient triple-negative breast cancer is therapeutically beneficial in human-in-mouse tumor models. The Journal of clinical investigation 20120402
A phase II study of cell cycle inhibitor UCN-01 in patients with metastatic melanoma: a California Cancer Consortium trial. Investigational new drugs 20120401
ATR-Chk1 signaling pathway and homologous recombinational repair protect cells from 5-fluorouracil cytotoxicity. DNA repair 20120301
Preclinical development of the novel Chk1 inhibitor SCH900776 in combination with DNA-damaging agents and antimetabolites. Molecular cancer therapeutics 20120201
Roles of phosphoinositide-dependent kinase-1 in α1B-adrenoceptor phosphorylation and desensitization. European journal of pharmacology 20120115
Bone morphogenetic protein (BMP)-4 and BMP-7 suppress granulosa cell apoptosis via different pathways: BMP-4 via PI3K/PDK-1/Akt and BMP-7 via PI3K/PDK-1/PKC. Biochemical and biophysical research communications 20120113
Phase I trial of 7-hydroxystaurosporine and fludararbine phosphate: in vivo evidence of 7-hydroxystaurosporine induced apoptosis in chronic lymphocytic leukemia. Leukemia & lymphoma 20111201
M2, a novel anthracenedione, elicits a potent DNA damage response that can be subverted through checkpoint kinase inhibition to generate mitotic catastrophe. Biochemical pharmacology 20111201
Poly(ADP-ribose) polymerase inhibition enhances p53-dependent and -independent DNA damage responses induced by DNA damaging agent. Cell cycle (Georgetown, Tex.) 20111201
Tauroursodeoxycholate (TUDCA) inhibits neointimal hyperplasia by suppression of ERK via PKCα-mediated MKP-1 induction. Cardiovascular research 20111101
Triggering of a novel intrinsic apoptosis pathway by the kinase inhibitor staurosporine: activation of caspase-9 in the absence of Apaf-1. FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20110901
A Phase 1 study of UCN-01 in combination with irinotecan in patients with resistant solid tumor malignancies. Cancer chemotherapy and pharmacology 20110601
Identification, in vitro activity and mode of action of phosphoinositide-dependent-1 kinase inhibitors as antifungal molecules. ACS chemical biology 20110520
Chk1 has an essential role in the survival of differentiated cortical neurons in the absence of DNA damage. Apoptosis : an international journal on programmed cell death 20110501
Determinants of mitotic catastrophe on abrogation of the G2 DNA damage checkpoint by UCN-01. Molecular cancer therapeutics 20110501
The DNA damage effector Chk1 kinase regulates Cdc14B nucleolar shuttling during cell cycle progression. Cell cycle (Georgetown, Tex.) 20110215
Phosphorylated hMSH6: DNA mismatch versus DNA damage recognition. Mutation research 20110110
Protein kinase C βII and δ/θ play critical roles in bone morphogenic protein-4-stimulated osteoblastic differentiation of MC3T3-E1 cells. Biochemical and biophysical research communications 20101203
Poly(ADP-ribose) polymerase 1 modulates the lethality of CHK1 inhibitors in carcinoma cells. Molecular pharmacology 20101101
PUMA induction by FoxO3a mediates the anticancer activities of the broad-range kinase inhibitor UCN-01. Molecular cancer therapeutics 20101101
Sodium butyrate with UCN-01 has marked antitumour activity against cervical cancer cells. Anticancer research 20101001
p53-dependent G(1) arrest in 1st or 2nd cell cycle may protect human cancer cells from cell death after treatment with ionizing radiation and Chk1 inhibitors. Cell proliferation 20100801
Structure-based and shape-complemented pharmacophore modeling for the discovery of novel checkpoint kinase 1 inhibitors. Journal of molecular modeling 20100701
Targeting slow-proliferating ovarian cancer cells. International journal of cancer 20100515
Cadmium-induced DNA damage triggers G(2)/M arrest via chk1/2 and cdc2 in p53-deficient kidney proximal tubule cells. American journal of physiology. Renal physiology 20100201
A role for Chk2 in DNA damage induced mitotic delays in human colorectal cancer cells. Cell cycle (Georgetown, Tex.) 20100115
A phase I trial of UCN-01 and prednisone in patients with refractory solid tumors and lymphomas. Cancer chemotherapy and pharmacology 20100101
Constitutive activation of the DNA damage signaling pathway in acute myeloid leukemia with complex karyotype: potential importance for checkpoint targeting therapy. Cancer research 20091115
Radiotherapy in conjunction with 7-hydroxystaurosporine: a multimodal approach with tumor pO2 as a potential marker of therapeutic response. Radiation research 20091101
Interaction with checkpoint kinase 1 modulates the recruitment of nucleophosmin to chromatin. Journal of proteome research 20091001
The G(2) DNA damage checkpoint: could this ancient regulator be the Achilles heel of cancer? Cancer biology & therapy 20090801
Cell cycle kinases as therapeutic targets for cancer. Nature reviews. Drug discovery 20090701
Phospho-p70S6K/p85S6K and cdc2/cdk1 are novel targets for diffuse large B-cell lymphoma combination therapy. Clinical cancer research : an official journal of the American Association for Cancer Research 20090301
Interruption of the Ras/MEK/ERK signaling cascade enhances Chk1 inhibitor-induced DNA damage in vitro and in vivo in human multiple myeloma cells. Blood 20080915
Chk1 inhibition activates p53 through p38 MAPK in tetraploid cancer cells. Cell cycle (Georgetown, Tex.) 20080701
G2/M checkpoint stringency is a key parameter in the sensitivity of AML cells to genotoxic stress. Oncogene 20080619
DNA damage-induced S phase arrest in human breast cancer depends on Chk1, but G2 arrest can occur independently of Chk1, Chk2 or MAPKAPK2. Cell cycle (Georgetown, Tex.) 20080601
Controlled release of a protein kinase inhibitor UCN-01 from liposomes influenced by the particle size. International journal of pharmaceutics 20080303
Phase I and pharmacokinetic study of UCN-01 in combination with irinotecan in patients with solid tumors. Cancer chemotherapy and pharmacology 20080301
Transient exposure of carcinoma cells to RAS/MEK inhibitors and UCN-01 causes cell death in vitro and in vivo. Molecular cancer therapeutics 20080301
Defective p53 signaling in p53 wild-type tumors attenuates p21waf1 induction and cyclin B repression rendering them sensitive to Chk1 inhibitors that abrogate DNA damage-induced S and G2 arrest. Molecular cancer therapeutics 20080201
Increased inducible nitric oxide synthase in lung carcinoma of smokers. Cancer 20080115
p53-dependent Chk1 phosphorylation is required for maintenance of prolonged G2 Arrest. Radiation research 20071201
AG490 influences UCN-01-induced cytotoxicity in glioma cells in a p53-dependent fashion, correlating with effects on BAX cleavage and BAD phosphorylation. Cancer letters 20071108
MEK1/2 inhibitors potentiate UCN-01 lethality in human multiple myeloma cells through a Bim-dependent mechanism. Blood 20070915
UCN-01 in combination with topotecan in patients with advanced recurrent ovarian cancer: a study of the Princess Margaret Hospital Phase II consortium. Gynecologic oncology 20070801
Statins synergistically potentiate 7-hydroxystaurosporine (UCN-01) lethality in human leukemia and myeloma cells by disrupting Ras farnesylation and activation. Blood 20070515
Phase I and pharmacokinetic study of 7-hydroxystaurosporine and carboplatin in advanced solid tumors. Clinical cancer research : an official journal of the American Association for Cancer Research 20070501
Inhibition of topoisomerase IIalpha and G2 cell cycle arrest by NK314, a novel benzo[c]phenanthridine currently in clinical trials. Molecular cancer therapeutics 20070501
[Research on cyclin-dependent kinase inhibitors: state of the art and perspective]. Zhonghua zhong liu za zhi [Chinese journal of oncology] 20070501
UCN-01 (7-hydroxystaurosporine) induces apoptosis and G1 arrest of both primary and metastatic oral cancer cell lines in vitro. Oral surgery, oral medicine, oral pathology, oral radiology, and endodontics 20070301
p53-deficient cells rely on ATM- and ATR-mediated checkpoint signaling through the p38MAPK/MK2 pathway for survival after DNA damage. Cancer cell 20070201
7-Hydroxystaurosporine may have a therapeutic role in treatment-resistant depression by inhibition of calcium/calmodulin-dependent protein kinase II. Medical hypotheses 20070101
Mechanisms of mitotic cell death induced by chemotherapy-mediated G2 checkpoint abrogation. Cancer research 20070101
Dissecting the roles of checkpoint kinase 1/CDC2 and mitogen-activated protein kinase kinase 1/2/extracellular signal-regulated kinase 1/2 in relation to 7-hydroxystaurosporine-induced apoptosis in human multiple myeloma cells. Molecular pharmacology 20061201
Modulation of cell cycle progression in human tumors: a pharmacokinetic and tumor molecular pharmacodynamic study of cisplatin plus the Chk1 inhibitor UCN-01 (NSC 638850). Clinical cancer research : an official journal of the American Association for Cancer Research 20061201
The Chk1-mediated S-phase checkpoint targets initiation factor Cdc45 via a Cdc25A/Cdk2-independent mechanism. The Journal of biological chemistry 20061013
Potentiation of the anticancer effect of valproic acid, an antiepileptic agent with histone deacetylase inhibitory activity, by the kinase inhibitor Staurosporine or its clinically relevant analogue UCN-01. British journal of cancer 20060522
p21CDKN1A allows the repair of replication-mediated DNA double-strand breaks induced by topoisomerase I and is inactivated by the checkpoint kinase inhibitor 7-hydroxystaurosporine. Oncogene 20060511
On the observed large interspecies overprediction of human clearance ('vertical allometry') of UCN-01: further support for a proposed model based on plasma protein binding. Journal of clinical pharmacology 20060401
Chk1 requirement for high global rates of replication fork progression during normal vertebrate S phase. Molecular and cellular biology 20060401
Pharmacodynamics of cytarabine alone and in combination with 7-hydroxystaurosporine (UCN-01) in AML blasts in vitro and during a clinical trial. Blood 20060315
Phase I trial of UCN-01 in combination with topotecan in patients with advanced solid cancers: a Princess Margaret Hospital Phase II Consortium study. Annals of oncology : official journal of the European Society for Medical Oncology 20060201
Transient exposure of mammary tumors to PD184352 and UCN-01 causes tumor cell death in vivo and prolonged suppression of tumor regrowth. Cancer biology & therapy 20051101
Two targets are better than one. Promising combination therapy to treat breast cancer. Cancer biology & therapy 20051101
A study of cytotoxic synergy of UCN-01 and flavopiridol in syngeneic pair of cell lines. Investigational new drugs 20050801
Molecular basis for G2 arrest induced by 2'-C-cyano-2'-deoxy-1-beta-D-arabino-pentofuranosylcytosine and consequences of checkpoint abrogation. Cancer research 20050801
Reducing the impact of binding of UCN-01 to human alpha1-acid glycoprotein by encapsulation in liposomes. Biological & pharmaceutical bulletin 20050701
The cyclin-dependent kinase inhibitor UCN-01 plus cisplatin in advanced solid tumors: a California cancer consortium phase I pharmacokinetic and molecular correlative trial. Clinical cancer research : an official journal of the American Association for Cancer Research 20050615
The farnesyltransferase inhibitor L744832 potentiates UCN-01-induced apoptosis in human multiple myeloma cells. Clinical cancer research : an official journal of the American Association for Cancer Research 20050615
Distinct roles for p53 transactivation and repression in preventing UCN-01-mediated abrogation of DNA damage-induced arrest at S and G2 cell cycle checkpoints. Oncogene 20050526
Drugging cell cycle kinases in cancer therapy. Current drug targets 20050501
Synergistic augmentation of rapamycin-induced autophagy in malignant glioma cells by phosphatidylinositol 3-kinase/protein kinase B inhibitors. Cancer research 20050415
Review of UCN-01 development: a lesson in the importance of clinical pharmacology. Journal of clinical pharmacology 20050401
Effect of 7-hydroxystaurosporine on glioblastoma cell invasion and migration. Acta pharmacologica Sinica 20050401
RNA silencing of checkpoint regulators sensitizes p53-defective prostate cancer cells to chemotherapy while sparing normal cells. Cancer research 20050401
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Phase I trial of the cyclin-dependent kinase inhibitor and protein kinase C inhibitor 7-hydroxystaurosporine in combination with Fluorouracil in patients with advanced solid tumors. Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20050320
Rapamycin and UCN-01 synergistically induce apoptosis in human leukemia cells through a process that is regulated by the Raf-1/MEK/ERK, Akt, and JNK signal transduction pathways. Molecular cancer therapeutics 20050301
Farnesyltransferase inhibitors interact synergistically with the Chk1 inhibitor UCN-01 to induce apoptosis in human leukemia cells through interruption of both Akt and MEK/ERK pathways and activation of SEK1/JNK. Blood 20050215
The mitotic spindle checkpoint is a critical determinant for topoisomerase-based chemotherapy. The Journal of biological chemistry 20050211
Synergistic stimulatory effect of 12-O-tetradecanoylphorbol-13-acetate and capsaicin on macrophage differentiation in HL-60 and HL-525 human myeloid leukemia cells. International journal of oncology 20050201
A phase I and pharmacokinetic study of short infusions of UCN-01 in patients with refractory solid tumors. Clinical cancer research : an official journal of the American Association for Cancer Research 20050115
Use of photoaffinity labeling and site-directed mutagenesis for identification of the key residue responsible for extraordinarily high affinity binding of UCN-01 in human alpha1-acid glycoprotein. The Journal of biological chemistry 20050114
The broad-range cyclin-dependent kinase inhibitor UCN-01 induces apoptosis in colon carcinoma cells through transcriptional suppression of the Bcl-x(L) protein. Oncogene 20050106
Phosphorylation of Plk1 at S137 and T210 is inhibited in response to DNA damage. Cell cycle (Georgetown, Tex.) 20050101
[Abrogation effect of UCN-01 on radiation-induced G2 phase arrest of tumor cells and its mechanism]. Ai zheng = Aizheng = Chinese journal of cancer 20050101
Blockage of cyclin cdk's, PKC and phosphoinositol 3-kinase pathways leads to augmentation of apoptosis in drug-resistant leukemia cells: evidence for interactive effects of flavopiridol, LY 294002, roscovitine,wortmannin and UCN-01. Anticancer research 20050101
Inhibitors of cyclin-dependent kinase modulators for cancer therapy. Progress in drug research. Fortschritte der Arzneimittelforschung. Progres des recherches pharmaceutiques 20050101
Enhancement of radiation cytotoxicity by UCN-01 in non-small cell lung carcinoma cells. Radiation research 20041201
Chk1 versus Cdc25: chking one's levels of cellular proliferation. Cell cycle (Georgetown, Tex.) 20041101
7-hydroxystaurosporine (UCN-01) inhibition of Akt Thr308 but not Ser473 phosphorylation: a basis for decreased insulin-stimulated glucose transport. Clinical cancer research : an official journal of the American Association for Cancer Research 20041101
Effects of alpha1-acid glycoprotein on the clinical pharmacokinetics of 7-hydroxystaurosporine. Clinical cancer research : an official journal of the American Association for Cancer Research 20041015
The dietary isothiocyanate sulforaphane targets pathways of apoptosis, cell cycle arrest, and oxidative stress in human pancreatic cancer cells and inhibits tumor growth in severe combined immunodeficient mice. Molecular cancer therapeutics 20041001
Combinations of 5-fluorouracil with UCN-01 or staurosporine. Nucleosides, nucleotides & nucleic acids 20041001
Implications of p53 in growth arrest and apoptosis on combined treatment of human Mammary epithelial cells with topotecan and UCN-01. Journal of experimental therapeutics & oncology 20041001
Potentiation of cytotoxicity of topoisomerase i poison by concurrent and sequential treatment with the checkpoint inhibitor UCN-01 involves disparate mechanisms resulting in either p53-independent clonogenic suppression or p53-dependent mitotic catastrophe. Cancer research 20040915
CHK1 and CHK2 are differentially involved in mismatch repair-mediated 6-thioguanine-induced cell cycle checkpoint responses. Molecular cancer therapeutics 20040901
Tryptophan residues play an important role in the extraordinarily high affinity binding interaction of UCN-01 to human alpha-1-acid glycoprotein. Pharmaceutical research 20040901
UCN-01 alters phosphorylation of Akt and GSK3beta and induces apoptosis in six independent human neuroblastoma cell lines. Journal of neurochemistry 20040801
In vitro combination treatment with perifosine and UCN-01 demonstrates synergism against prostate (PC-3) and lung (A549) epithelial adenocarcinoma cell lines. Clinical cancer research : an official journal of the American Association for Cancer Research 20040801
Time to disease progression to evaluate a novel protein kinase C inhibitor, UCN-01, in renal cell carcinoma. Cancer 20040701
Rapid degradation of Cdt1 upon UV-induced DNA damage is mediated by SCFSkp2 complex. The Journal of biological chemistry 20040625
Persistent activation of the Akt pathway in head and neck squamous cell carcinoma: a potential target for UCN-01. Clinical cancer research : an official journal of the American Association for Cancer Research 20040615
Abrogation of Chk1-mediated S/G2 checkpoint by UCN-01 enhances ara-C-induced cytotoxicity in human colon cancer cells. Acta pharmacologica Sinica 20040601
Mismatch repair-dependent G2 checkpoint induced by low doses of SN1 type methylating agents requires the ATR kinase. Genes & development 20040601
UCN-01-induced cell cycle arrest requires the transcriptional induction of p21(waf1/cip1) by activation of mitogen-activated protein/extracellular signal-regulated kinase kinase/extracellular signal-regulated kinase pathway. Cancer research 20040515
Metabolism of UCN-01 in isolated perfused rat liver: role of Mrp2 in the biliary excretion of glucuronides. Oncology reports 20040501
Interruption of the NF-kappaB pathway by Bay 11-7082 promotes UCN-01-mediated mitochondrial dysfunction and apoptosis in human multiple myeloma cells. Blood 20040401
Pheophorbide a is a specific probe for ABCG2 function and inhibition. Cancer research 20040215
Cell-cycle targeted therapies. The Lancet. Oncology 20040101
Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) promotes mitochondrial dysfunction and apoptosis induced by 7-hydroxystaurosporine and mitogen-activated protein kinase kinase inhibitors in human leukemia cells that ectopically express Bcl-2 and Bcl-xL. Molecular pharmacology 20031201
The expression of retinoblastoma and Sp1 is increased by low concentrations of cyclin-dependent kinase inhibitors. European journal of biochemistry 20031201
Induction by staurosporine of hepatocyte growth factor production in human skin fibroblasts independent of protein kinase inhibition. Biochemical pharmacology 20031101
Cell cycle modulators for the treatment of lung malignancies. Clinical lung cancer 20031101
Structural basis for UCN-01 (7-hydroxystaurosporine) specificity and PDK1 (3-phosphoinositide-dependent protein kinase-1) inhibition. The Biochemical journal 20031015
Induction of colon cancer cell death by 7-hydroxystaurosporine (UCN-01) is associated with increased p38 MAPK and decreased Bcl-xL. Anti-cancer drugs 20031001
Synergistic antileukemic interactions between 17-AAG and UCN-01 involve interruption of RAF/MEK- and AKT-related pathways. Blood 20030901
An overactivated ATR/CHK1 pathway is responsible for the prolonged G2 accumulation in irradiated AT cells. The Journal of biological chemistry 20030815
Survival-signaling pathway as a promising target for cancer chemotherapy. Cancer chemotherapy and pharmacology 20030701
Novel direct and indirect cyclin-dependent kinase modulators for the prevention and treatment of human neoplasms. Cancer chemotherapy and pharmacology 20030701
Cell cycle-dependent potentiation of cisplatin by UCN-01 in non-small-cell lung carcinoma. Cancer chemotherapy and pharmacology 20030401
Human replication protein Cdc6 prevents mitosis through a checkpoint mechanism that implicates Chk1. The EMBO journal 20030203
Bryostatin 1 and UCN-01 potentiate 1-beta-D-arabinofuranosylcytosine-induced apoptosis in human myeloid leukemia cells through disparate mechanisms. Molecular pharmacology 20030101
[Abrogation of radiation-induced G2 arrest and radiosensitization by 7-hydroxystaurosporine (UCN-01) in human nasopharyngeal carcinoma cell line]. Ai zheng = Aizheng = Chinese journal of cancer 20030101
Potentiation of DNA-damage-induced cytotoxicity by G2 checkpoint abrogators. Current medicinal chemistry. Anti-cancer agents 20030101
Cyclin-dependent kinase modulators studied at the NCI: pre-clinical and clinical studies. Current medicinal chemistry. Anti-cancer agents 20030101
Cisplatin-induced ubiquitination of RNA polymerase II large subunit and suppression of induction by 7-hydroxystaurosporine (UCN-01). Oncology reports 20030101
Combined antitumor activity of 7-hydroxystaurosporine (UCN-01) and tamoxifen against human breast carcinoma in vitro and in vivo. Breast cancer (Tokyo, Japan) 20030101
Structural basis for Chk1 inhibition by UCN-01. The Journal of biological chemistry 20021129
Combined treatment with the checkpoint abrogator UCN-01 and MEK1/2 inhibitors potently induces apoptosis in drug-sensitive and -resistant myeloma cells through an IL-6-independent mechanism. Blood 20021101
Antitumor activity of UCN-01 in carcinomas of the head and neck is associated with altered expression of cyclin D3 and p27(KIP1). Clinical cancer research : an official journal of the American Association for Cancer Research 20021101
UCN-01 inhibits p53 up-regulation and abrogates gamma-radiation-induced G(2)-M checkpoint independently of p53 by targeting both of the checkpoint kinases, Chk2 and Chk1. Cancer research 20021015
A novel indolocarbazole, ICP-1, abrogates DNA damage-induced cell cycle arrest and enhances cytotoxicity: similarities and differences to the cell cycle checkpoint abrogator UCN-01. Molecular cancer therapeutics 20021001
Cyclin-dependent kinases as new targets for the prevention and treatment of cancer. Hematology/oncology clinics of North America 20021001
Inhibition of cyclin-dependent kinase 2 by the Chk1-Cdc25A pathway during the S-phase checkpoint activated by fludarabine: dysregulation by 7-hydroxystaurosporine. Molecular pharmacology 20020901
7-hydroxystaurosporine (UCN-01) and ionizing radiation combine to inhibit the growth of Bcl-2-overexpressing U937 leukemia cells through a non-apoptotic mechanism. International journal of oncology 20020801
Hematologic malignancies: new developments and future treatments. Seminars in oncology 20020801
Abrogation of the radiation-induced G2 checkpoint by the staurosporine derivative UCN-01 is associated with radiosensitisation in a subset of colorectal tumour cell lines. British journal of cancer 20020729
Abrogation of the S phase DNA damage checkpoint results in S phase progression or premature mitosis depending on the concentration of 7-hydroxystaurosporine and the kinetics of Cdc25C activation. The Journal of biological chemistry 20020719
7-Hydroxystaurosporine (UCN-01) preferentially sensitizes cells with a disrupted TP53 to gamma radiation in lung cancer cell lines. Radiation research 20020701
7-Hydroxystaurosporine-induced apoptosis in 9L glioma cells provides an effective antigen source for dendritic cells and yields a potent vaccine strategy in an intracranial glioma model. Neurosurgery 20020601
Seventy-two hour continuous infusion flavopiridol in relapsed and refractory mantle cell lymphoma. Leukemia & lymphoma 20020401
Interference with PDK1-Akt survival signaling pathway by UCN-01 (7-hydroxystaurosporine). Oncogene 20020307
Radiation-induced phosphorylation of Chk1 at S345 is associated with p53-dependent cell cycle arrest pathways. Neoplasia (New York, N.Y.) 20020301
Biochemical and molecular effects of UCN-01 in combination with 5-fluorodeoxyuridine in A431 human epidermoid cancer cells. Anti-cancer drugs 20020301
Carcinogen-induced S-phase arrest is Chk1 mediated and caffeine sensitive. Cell growth & differentiation : the molecular biology journal of the American Association for Cancer Research 20020201
UCN-01 (7-hydroxystaurosporine) inhibits DNA repair and increases cytotoxicity in normal lymphocytes and chronic lymphocytic leukemia lymphocytes. Molecular cancer therapeutics 20020201
Protein kinase C inhibitors. Current oncology reports 20020101
Influence of G2 arrest on the cytotoxicity of DNA topoisomerase inhibitors toward human carcinoma cells with different p53 status. Acta biochimica Polonica 20020101
The cell cycle as a target for cancer therapy: basic and clinical findings with the small molecule inhibitors flavopiridol and UCN-01. The oncologist 20020101
UCN-01 (7-hydroxystaurosporine) inhibits the growth of human breast cancer xenografts through disruption of signal transduction. Breast cancer (Tokyo, Japan) 20020101
Combining phorbol ester (PMA) with UCN-01: fueling fire with water. Cell cycle (Georgetown, Tex.) 20020101
UCN-01 (7-hydroxystauorsporine) blocks PMA-induced maturation and reciprocally promotes apoptosis in human myelomonocytic leukemia cells (U937). Cell cycle (Georgetown, Tex.) 20020101
Inhibitors of MEK1/2 interact with UCN-01 to induce apoptosis and reduce colony formation in mammary and prostate carcinoma cells. Cancer biology & therapy 20020101
CHK and MEK inhibitors team up to trigger cancer cell suicide. Cancer biology & therapy 20020101
Independent antitumor spectrum of UCN-01 (7-hydroxystaurosporine) against gastric and colorectal cancers as detected by MTT assay. Anticancer research 20020101
Coadministration of UCN-01 with MEK1/2 inhibitors potently induces apoptosis in BCR/ABL+ leukemia cells sensitive and resistant to ST1571. Cancer biology & therapy 20020101
Beyond directed therapeutics--are two drugs always better than one? Cancer biology & therapy 20020101
Development of a simplified, sensitive high-performance liquid chromatographic method using fluorescence detection to determine the concentration of UCN-01 in human plasma. Journal of chromatography. B, Biomedical sciences and applications 20010905
Blocking Chk1 expression induces apoptosis and abrogates the G2 checkpoint mechanism. Neoplasia (New York, N.Y.) 20010901
Abrogation of the Chk1-mediated G(2) checkpoint pathway potentiates temozolomide-induced toxicity in a p53-independent manner in human glioblastoma cells. Cancer research 20010801
Susceptibility of thyroid cancer cells to 7-hydroxystaurosporine-induced apoptosis correlates with Bcl-2 protein level. Thyroid : official journal of the American Thyroid Association 20010801
UCN-01 dose-dependent inhibition of normal hyperproliferative cells in mice. International journal of oncology 20010701
Pharmacological inhibitors of the mitogen-activated protein kinase (MAPK) kinase/MAPK cascade interact synergistically with UCN-01 to induce mitochondrial dysfunction and apoptosis in human leukemia cells. Cancer research 20010701
Protein binding alters the activity of suramin, carboxyamidotriazole, and UCN-01 in an ex vivo rat aortic ring angiogenesis assay. Clinical cancer research : an official journal of the American Association for Cancer Research 20010701
UCN-01 induces cytotoxicity toward human CLL cells through a p53-independent mechanism. Experimental hematology 20010601
UCN-01 (7-hydoxystaurosporine) inhibits in vivo growth of human cancer cells through selective perturbation of G1 phase checkpoint machinery. Japanese journal of cancer research : Gann 20010501
Phase I trial of 72-hour continuous infusion UCN-01 in patients with refractory neoplasms. Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20010415
Regulation of the G2/M transition by p53. Oncogene 20010405
Localization of human Cdc25C is regulated both by nuclear export and 14-3-3 protein binding. Oncogene 20010405
Resistance to growth inhibitory and apoptotic effects of phorbol ester and UCN-01 in aggressive cancer cell lines. International journal of oncology 20010401
[CDK inhibitors for therapy of cancer]. Nihon rinsho. Japanese journal of clinical medicine 20010401
UCN-01 suppresses E2F-1 mediated by ubiquitin-proteasome-dependent degradation. Clinical cancer research : an official journal of the American Association for Cancer Research 20010301
S-Phase arrest by nucleoside analogues and abrogation of survival without cell cycle progression by 7-hydroxystaurosporine. Cancer research 20010201
Interactions between 2-fluoroadenine 9-beta-D-arabinofuranoside and the kinase inhibitor UCN-01 in human leukemia and lymphoma cells. Clinical cancer research : an official journal of the American Association for Cancer Research 20010201
UCN-01 Kyowa Hakko Kogyo Co. Current opinion in investigational drugs (London, England : 2000) 20010201
Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer's disease. A property common to most cyclin-dependent kinase inhibitors? The Journal of biological chemistry 20010105
Development of cyclin-dependent kinase modulators as novel therapeutic approaches for hematological malignancies. Leukemia 20010101
Pharmacokinetics, distribution, metabolism and excretion of. Cancer chemotherapy and pharmacology 20010101
Abrogation of G2 checkpoint specifically sensitize p53 defective cells to cancer chemotherapeutic agents. Anticancer research 20010101
Tissue distribution and plasma pharmacokinetics of UCN-01 at steady-state and following bolus administration in rats: influence of human alpha1-acid glycoprotein binding. Anticancer research 20010101
Protein kinase inhibitors flavopiridol and 7-hydroxy-staurosporine down-regulate antiapoptosis proteins in B-cell chronic lymphocytic leukemia. Blood 20000715
The radiosensitizing agent 7-hydroxystaurosporine (UCN-01) inhibits the DNA damage checkpoint kinase hChk1. Cancer research 20000415
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