A prodrug for the Hsp90 inhibitor

PF-04929113 – 25 mg

Brand:
Cayman
CAS:
908115-27-5
Storage:
-20
UN-No:
Non-Hazardous - /

PF-04929113 is a prodrug for the Hsp90 inhibitor, PF-04958473 (SNX-2112; Item No. 22359), which binds both Hsp90α and Hsp90β with an IC50 value of 30 nM.{31149,31150} The prodrug, PF-04929113, is rapidly absorbed and converted into the active inhibitor after oral administration.{31150} The active inhibitor causes degradation of Hsp90 client proteins, including HER2, and reduces phosphorylation of downstream kinases, including Akt and ERK1/2, leading to apoptosis in cancer cells.{31149,31152} Oral administration of the prodrug, PF-04929113, reduces tumor growth and prolongs survival in mouse models of multiple myeloma and prostate cancer.{31152,31151}  

 

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Description

A prodrug for the Hsp90 inhibitor, PF-04958473 (SNX-2112), which binds both Hsp90α and Hsp90β with an IC50 value of 30 nM; reduces tumor growth and prolongs survival in mouse models of multiple myeloma and prostate cancer when given orally

Formal name: glycine, trans-4-[[2-(aminocarbonyl)-5-[4,5,6,7-tetrahydro-6,6-dimethyl-4-oxo-3-(trifluoromethyl)-1H-indazol-1-yl]phenyl]amino]cyclohexyl ester

Synonyms:  SNX-5422

Molecular weight: 521.5

CAS: 908115-27-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Heat Shock Proteins||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cell Biology|Cellular Chaperones

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