AST-487

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP21589CAS No. ：630124-46-8Purity：98%

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CAS No.	630124-46-8	Cat. No.	BCP21589
Name	AST-487
Synonyms	NVPAST487; AST 487; AST487;NVP-AST-487;
SMILES	CCN1CCN(CC1)CC2=C(C=C(C=C2)NC(=O)NC3=CC=C(C=C3)OC4=NC=NC(=C4)NC)C(F)(F)F
Chemical Name
Formula	C26H30F3N7O2	M. Wt	529.56
Purity	98%	Storage	Store at 4-8°C
Description	AST487, also known as NVP- AST487, is a RET kinase inhibitor/FLT3 inhibitor. 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 has an IC(50) of 0.88 mumol/L on RET kinase, inhibits 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. NVP- AST487 inhibited calcitonin gene expression in vitro in TT cells, in part, through decreased gene transcription.