AST487 (NVP- AST487)

Description: AST487 (also known as NVP- AST487) is a novel and potent inhibitor of RET kinase with IC50 of 880 nM. The RET kinase has emerged as a promising target for the therapy of medullary thyroid cancers (MTC) and of a subset of papillary thyroid cancers. NVP-AST487, a N, N'-diphenyl urea with an IC(50) of 0.88 mumol/L on RET kinase, inhibited RET autophosphorylation and activation of downstream effectors, and potently inhibited the growth of human thyroid cancer cell lines with activating mutations of RET but not of lines without RET mutations. NVP-AST487 induced a dose-dependent growth inhibition of xenografts of NIH3T3 cells expressing oncogenic RET, and of the MTC cell line TT in nude mice.

References: Cancer Res. 2007 Jul 15; 67(14):6956-64.

Synonym: AST 487; AST487; AST-487; NVP AST487; NVP AST-487; NVP AST 487; NVP-AST487; NVP-AST-487; NVP-AST 487

.Chemical Name: 1-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-(4-((6-(methylamino)pyrimidin-4-yl)oxy)phenyl)urea