"目录号: HY-15263
Cell Cycle/DNA DamageMetabolic Enzyme/Protease-
Retaspimycin(IPI 504)是HSP90抑制剂，具有抗增殖和抗肿瘤活性。
HSP
相关产品
17-AAG-Triptolide-NVP-AUY922-Ganetespib-Geldanamycin-Teprenone-Rocaglamide-VER-155008-AT13387-Retaspimycin Hydrochloride-Alvespimycin hydrochloride-Debio 0932-BIIB021-PU-H71-NVP-HSP990-
生物活性
Description
Retaspimycin(IPI 504) is a small-molecule inhibitor of heat shock protein 90 (HSP90) with antiproliferative and antineoplastic activities. IC50 Value:Target: HSPRetaspimycin binds to and inhibits the cytosolic chaperone functions of HSP90, which maintains the stability and functional shape of many oncogenic signaling proteins and may be overexpressed or overactive in tumor cells. Retaspimycin-mediated inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins in susceptible tumor cell populations, which may result in the induction of apoptosis.
Clinical Trial
NCT01362400
Infinity Pharmaceuticals, Inc.
Non Small Cell Lung Cancer
May 2011
Phase 2
NCT00564928
Infinity Pharmaceuticals, Inc.
Prostate Cancer-Prostatic Neoplasms-Cancer of the Prostate
November 2007
Phase 2
NCT00606814
Infinity Pharmaceuticals, Inc.
Solid Tumors
December 2007
Phase 1
NCT00113204
Infinity Pharmaceuticals, Inc.
Multiple Myeloma
June 2005
Phase 1
NCT00817362
Infinity Pharmaceuticals, Inc.
Breast Cancer-HER2 Positive Breast Cancer-Metastatic Breast Cancer-Cancer of the Breast
March 2009
Phase 2
NCT00627419
Infinity Pharmaceuticals, Inc.
Metastatic Melanoma
February 2008
Phase 2
NCT00276302
Infinity Pharmaceuticals, Inc.
Gastrointestinal Stromal Tumors-Soft Tissue Sarcomas
December 2005
Phase 1
NCT00627627
MedImmune LLC
Breast Cancer
April 2008
Phase 1-Phase 2
NCT00969917
Infinity Pharmaceuticals, Inc.
Dedifferentiated Liposarcoma
January 2010
Phase 2
NCT01427946
Infinity Pharmaceuticals, Inc.
Non-small Cell Lung Cancer
July 2011
Phase 1-Phase 2
NCT00431015
Infinity Pharmaceuticals, Inc.
Lung Cancer
January 2007
Phase 1-Phase 2
NCT00688766
Infinity Pharmaceuticals, Inc.-MedImmune LLC-AstraZeneca
Gastrointestinal Stromal Tumors
August 2008
Phase 3
NCT01228435
Massachusetts General Hospital-Dana-Farber Cancer Institute-Infinity Pharmaceuticals, Inc.
Lung Cancer-Stage IIIb Lung Cancer-Stage IV Lung Cancer
October 2010
Phase 2
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References
[1].Oh WK, Galsky MD, Stadler WM, Srinivas S, Chu F, Bubley G, Goddard J, Dunbar J, Ross RW.Multicenter phase II trial of the heat shock protein 90 inhibitor, retaspimycin hydrochloride (IPI-504), in patients with castration-resistant prostate cancer. Urolog
[2].Hanson BE, Vesole DH. Retaspimycin hydrochloride (IPI-504): a novel heat shock protein inhibitor as an anticancer agent. Expert Opin Investig Drugs. 2009 Sep;18(9):1375-83.
[3].Siegel D, Jagannath S, Vesole DH, Borello I, Mazumder A, Mitsiades C, Goddard J, Dunbar J, Normant E, Adams J, Grayzel D, Anderson KC, Richardson P. A phase 1 study of IPI-504 (retaspimycin hydrochloride) in patients with relapsed or relapsed and refract
[4].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 By Douglas, Mark; Lim, Alice R.; Porter, James R.; West, Kip; Pink, Melissa M.; Ge, Jie; Wylie, Andrew A.;
[5].A mechanistic and structural analysis of the inhibition of the 90-kDa heat shock protein by the benzoquinone and hydroquinone ansamycins By Reigan, Philip; Siegel, David; Guo, Wenchang; Ross, David From Molecular Pharmacology (2011), 79(5), 823-832.