A Hsp90 inhibitor (IC50 = 21 nM in a FP binding assay) that prevents the proliferation of a range of human cancer cell lines in vitro (GI50s ~ 9nM); 50 mg/kg inhibits tumor growth in a human colon cancer xenograft model by ~50% compared to vehicle controls

NVP-AUY922 – 10 mg

Brand:
Cayman
CAS:
747412-49-3
Storage:
-20
UN-No:
Non-Hazardous - /

Hsp90 is a molecular chaperone of many different kinases, transcription factors, and hormone receptors involved in signal transduction, cell cycle regulation, and apoptosis. In addition to its important function in normal cell homeostasis, a high affinity form of Hsp90 is prevalent in tumor cells. Hsp90 inhibition has been associated with the degradation of oncogenic client proteins. NVP-AUY922 is a Hsp90 inhibitor (IC50 = 21 nM in a FP binding assay) that prevents the proliferation of a range of human cancer cell lines in vitro with GI50s averaging 9 nM.{15809} In a human colon cancer xenograft model, 50 mg/kg NVP-AUY922 inhibits tumor growth by ~50% compared to vehicle controls.{15809} Unlike some first generation Hsp90 inhibitors that are quickly glucuronidated, NVP-AUY922 is retained in tumors in vivo when administered at 4 mg/kg i.p. by cassette dosing in tumor-bearing mice.{15809}  

 

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SKU: 10012698 - 10 mg Category:

Description

A Hsp90 inhibitor (IC50 = 21 nM in a FP binding assay) that prevents the proliferation of a range of human cancer cell lines in vitro (GI50s ~ 9nM); 50 mg/kg inhibits tumor growth in a human colon cancer xenograft model by ~50% compared to vehicle controls

Formal name: 5-[2,4-dihydroxy-5-(1-methylethyl)phenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide

Synonyms:  VER 52296

Molecular weight: 465.5

CAS: 747412-49-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Heat Shock Proteins||Research Area|Cancer

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