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AST 487
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AST 487图片
CAS NO:630124-46-8
规格:98%
分子量:529.56
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
RET kinase inhibitor
CAS:630124-46-8
分子式:C26H30F3N7O2
分子量:529.56
纯度:98%
存储:Store at -20°C

Background:

AST487 is an inhibitor of RET kinase with IC50 value of 0.88μM [1].


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 [1].


参考文献:
[1] Nagako Akeno-Stuart, Michelle Croyle, Jeffrey A. Knauf, et al. The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells. Cancer Res. 2007, 67:6956-6964.