An inhibitor of RET (IC50 = 0.88 µM)

AST-487 – 1 mg

Brand:
Cayman
CAS:
630124-46-8
Storage:
-20
UN-No:
Non-Hazardous - /

AST-487 is an inhibitor of RET (IC50 = 0.88 µM), FLT3 (Ki = 0.52 µM), KDR (IC50 = 0.17 µM), c-Abl (IC50 = 0.02 µM), and c-Kit (IC50 = 0.5 µM).{31675,31676} It has been shown to inhibit RET autophosphorylation and activation of downstream effectors and to prevent the growth of human thyroid cancer cell lines with activating mutations of RET but not of lines without RET mutations.{31675} In xenografts of NIH3T3 cells expressing oncogenic RET and of the MTC cell line TT in nude mice, AST-487 dose dependently inhibited tumor growth.{31675} It also demonstrates antiproliferative effects on primary cells from acute myelocytic leukemia patients and on cell lines expressing FLT3-ITD or FLT3 kinase domain point mutants.{31675}  

 

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Description

An inhibitor of RET (IC50 = 0.88 µM), FLT3 (Ki = 0.12 µM), KDR, c-Abl, and c-Kit; demonstrates antiproliferative activity in various cancer cells, including those with RET or FLT3 mutations

Formal name: N-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-N’-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]-urea

Synonyms:  NVP-AST-487

Molecular weight: 529.6

CAS: 630124-46-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Abl Family & Bcr-Abl||Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Kinase Inhibitors|VEGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Abl family & Bcr-Abl Signaling||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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