Synonyms: 1-(4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-(4-(6-(methylamino)pyrimidin-4-yloxy)phenyl)urea; AST 487; AST-487; N-[4-[(4-Ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-N'-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]urea; NVP-AST 487; NVP-AST-487; NVP-AST487
Molecular Formula: C26H30F3N7O2
Molecular Weight: 529.56
Linear Structural Formula: C26H30F3N7O2
MDL Number: MFCD11983171
Purity: >=98% (HPLC)
Storage: -20C
Biochem Physiol Actions: AST487 is an orally available type II tyrosine kinase inhibitor (TKI) that exhibits potent antiproliferation activity against FLT3, RET, PDGFR1, but not BRAF, oncogenic fusions/mutations-driven growth (IC50 = 1.8 nM/FLT3-ITD BaF3, 5.1 nM/FLT3 D835I BaF3, 9-27 nM/TEL-PDGFR1 & PTC3-RET BaF3,<1 nm lt3-itd-expressing mv4-11 & molm-13) via binding tablizing target kinases in the inactive dfg-out conformation. ast487 effectively suppresses ret- (nih3t3-retc634w & human medullary thyroid cancer (mtc) tt cells) and flt3-itd-driven (mv4-11) tumor growth in mice in vivo (20-50 mg g ay p.o.).<>