AST487
SIGMA/SML2363 - ≥98% (HPLC)
Synonym: 1-
CAS Number: 630124-46-8
Empirical Formula (Hill Notation): C26H30F3N7O2
Molecular Weight: 529.56
MDL Number: MFCD11983171
Linear Formula: C26H30F3N7O2
Product Type: Chemical
assay | ≥98% (HPLC) |
color | white to beige |
form | powder |
SMILES string | CCN1CCN(CC2=C(C(F)(F)F)C= |
solubility | DMSO: 2 mg/mL, clear |
storage temp. | −20°C |
Biochem/physiol Actions: | AST487 is a N,N′-diphenyl urea, which inhibits growth and calcitonin gene expression in medullary thyroid cancer cells. |
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/FLT3-ITD-expressing MV4-11 & MOLM-13) via binding/stablizing 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/kg/day p.o.). |
WGK Germany | WGK 3 |
Flash Point(F) | Not applicable |
Flash Point(C) | Not applicable |
Purity | ≥98% (HPLC) |
Storage Temp. | −20°C |
UNSPSC | 12352200 |