AUY922 (NVP-AUY922)

溶解性

In vitro (25℃) DMSO 93 mg/mL heating (199.76 mM)

効能

抗悪性腫瘍薬, 熱ショックタンパク質阻害薬

説明

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. In a human colon cancer xenograft model, 50 mg/kg NVP-AUY922 inhibits tumor growth by ~50% compared to vehicle controls. 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.

定義

ChEBI: A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-(2,4-dihydroxy-5-isopropylphenyl)-4-[4-(morpholin-4-ylmethyl)phenyl]-1,2-oxazole-3-carboxylic acid with the amino group of ethylamine.