产品说明书

SB-590885

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Chemical Structure| 405554-55-4 同义名 : -
CAS号 : 405554-55-4
货号 : A720977
分子式 : C27H27N5O2
纯度 : 99%+
分子量 : 453.536
MDL号 : MFCD16038645
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 9 mg/mL(19.84 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • B-Raf

    B-Raf, Ki:0.16 nM
描述 The RAS/RAF signaling pathway is an important mediator of tumor cell proliferation and angiogenesis. Among them, B-RAF is the most frequently mutated protein kinase in human cancers. SB-590885 is a selective Raf kinase inhibitor with Kiapp value of 0.16nM for B-Raf (measured by kinase activity), 11-fold greater selectivity over c-Raf (Kiapp=1.72nM), with little inhibition to other human kinases. Treatment with SB-590885, 2μM for 1h, inhibited ERK phosphorylation in Colo205 and HT29 cell lines, as well as potently and preferentially inhibited ERK phosphorylation and proliferation in tumor cells expressing B-RafV600E. Prolonged exposure to SB-590885, at dose ranging 0.1-10μM for 72h, inhibited cellular transformation and proliferation in three-dimensional culture. Daily administration of SB-590885 at dose of 50m/kg, i.p., decreased tumorigenesis in murine xenografts established from mutant B-Raf-expressing A375P melanoma cells[1].
作用机制 SB-590885 occupies the ATP-binding pocket of B-Raf and stabilizes the oncogenic B-Raf kinase domain in an active configuration.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

11.02mL

2.20mL

1.10mL

22.05mL

4.41mL

2.20mL
参考文献

[1]King AJ, Patrick DR, et al. Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885. Cancer Res. 2006 Dec 1;66(23):11100-5.