"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.