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AST487

SIGMA/SML2363 - ≥98% (HPLC)

Synonym: 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

CAS Number: 630124-46-8
Empirical Formula (Hill Notation): C26H30F3N7O2
Molecular Weight: 529.56
MDL Number: MFCD11983171
Linear Formula: C26H30F3N7O2
Product Type: Chemical
Catalog Number PKG Qty. Price Quantity
45-SML2363-5MG 5 mg
 $99.00
1/EA		 Add To Favorites
45-SML2363-25MG 25 mg
 $399.00
1/EA		 Add To Favorites

 

assay ≥98% (HPLC)
color white to beige
form powder
SMILES string CCN1CCN(CC2=C(C(F)(F)F)C=C(NC(NC3=CC=C(OC4=NC=NC(NC)=C4)C=C3)=O)C=C2)CC1
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 &amp; 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

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