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AST 487
Cat No.
CEI-1220
Description
AST487 is an inhibitor of RET kinase with IC50 value of 0.88 μM.
Product Overview
AST487 is an inhibitor of RET kinase with IC50 value of 0.88μM. AST487 belongs to the N,N'-diphenyl urea class. It inhibit the activity of RET kinase as well as many other kinases(such as KDR, Flt-3 and c-Kit) in vitro. In the cell assay, the inhibition effect of AST487 is displayed both in PC-RET/PTC3 cells and TT cells, which harbor an endogenous activating point mutation of RET (RETC634W). AST487 decreases RET autophosphorylation and activation of PLCγ and ERK with a dose-dependent manner. Additionally, AST487 is also found to inhibit the growth of human thyroid cancer cell lines with RET, but not BRAF mutations. It supports the selectivity of AST487 for RET. In vivo assay shows that AST487 causes significant reductions in the size of NIH3T3-RETC634W xenografts with doses >30 mg/kg/d and oral administration of AST487 at 50 or 30 mg/kg/d decreases mean tumor volume in mice.
CAS No.
630124-46-8
Molecular Weight
529.56
Purity
0.98
Storage
Store at -20°C
Synonyms
NVP-AST 487
Targets
RET kinase
IC50
0.88 μM
Molecular Formula
C26H30F3N7O2
Chemical Name
1-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[6-(methylamino)pyrimidin-4-yl]oxyphenyl]urea
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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