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AST 487 Chemical Structure
|Product name: AST 487|
|Cat. No.: HY-15002|
AST487(NVP-AST487) is a Ret kinase inhibitor/FLT3 inhibitor with IC50 of 0.88 uM for Ret.
IC50 value: 0.88 uM
AST 487 displays high selectivity and potency toward FLT3 as a molecular target, and which could potentially be used to override drug resistance in AML. NVP-AST487 has an IC(50) of 0.88 mumol/L on RET kinase, inhibits RET autophosphorylation and activation of downstream effectors, and potently inhibited the growth of human thyroid cancer cell lines with activating mutations of RET but not of lines without RET mutations. NVP-AST487 induced a dose-dependent growth inhibition of xenografts of NIH3T3 cells expressing oncogenic RET, and of the MTC cell line TT in nude mice. NVP-AST487 inhibited calcitonin gene expression in vitro in TT cells, in part, through decreased gene transcription.
|M.Wt||529.56||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||1.8884 mL||9.4418 mL||18.8836 mL|
|5 mM||0.3777 mL||1.8884 mL||3.7767 mL|
|10 mM||0.1888 mL||0.9442 mL||1.8884 mL|
. Weisberg, Ellen; Roesel, Johannes; Furet, Pascal et al. Antileukemic effects of novel first-and second-generation FLT3 inhibitors: structure-affinity comparison. Genes & Cancer (2010), 1(10), 1021-1032.
. Akeno-Stuart, Nagako; Croyle, Michelle; Knauf, Jeffrey A. et al. The RET Kinase Inhibitor NVP-AST487 Blocks Growth and Calcitonin Gene Expression through Distinct Mechanisms in Medullary Thyroid Cancer Cells. Cancer Research (2007), 67(14), 6956-6964.
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