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8-(2-chloro-3,4,5-trimethoxy-benzyl)-9-pent-4-ylnyl-9h-purin-6-ylamine

Development stage
Preclinical
Lead developer
Vernalis
Modality
Small Molecules
01

Overview

8-(2-chloro–3,4,5-trimethoxy-benzyl)-9-pent–4-ylnyl–9H–purin–6–ylamine is a synthetic small molecule belonging to the class of 6‑aminopurines. It is an experimental compound developed as a purine-based inhibitor of heat shock protein Hsp90 (specifically Hsp90-alpha). By binding to the N-terminal ATP-binding domain of Hsp90-alpha and inhibiting its ATPase activity, it disrupts the chaperone function required for stability and function of multiple oncogenic client proteins. This leads to degradation of proteins such as Raf‑1 kinase and ErbB2/HER2 and results in antitumor effects. The compound has been studied primarily in preclinical settings as an antineoplastic agent targeting cancer cell growth via Hsp90 inhibition[3][7].

Other names
8-(2-chloro-3,4,5-trimethoxy-benzyl)-9-pent-4-ylnyl-9h-purin-6-yalmine8-[2-chloro-3,4,5-trimethoxyphenyl)methyl]-9-(pent-4-yn-1-yl)-9H-purin-6-aminaDB04505DB-04505DB 04505
02

Targets

HSP90 (Heat shock protein 90 chaperone complex)

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