|5-(2-(4-(2-(二甲基氨基)乙氧基)苯基)-5-(吡啶-4-基)-1H-咪唑-4-基)-2,3-二氢-1H-茚-1-酮肟|CsnPharm

CAS No.: 405554-55-4

5-(2-(4-(2-(Dimethylamino)ethoxy)phenyl)-5-(pyridin-4-yl)-1H-imidazol-4-yl)-2,3-dihydro-1H-inden-1-one oxime Catalog No. CSN16576

SB-590885 is a potent B-Raf inhibitor with Ki of 0.16 nM, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 C-Raf

Ki:1.76nM B-Raf

Ki:0.16nM
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 Ki_app value of 0.16nM for B-Raf (measured by kinase activity), 11-fold greater selectivity over c-Raf (Ki_app=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-Raf^V600E. 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]
动物研究
剂量
Nude Mice: 50 mg/kg^[1] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Nude Mice: 50 mg/kg^[1] (i.p.)
给药途径	i.p.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2049 mL
- 11.0245 mL
- 22.0490 mL
- 5 mM
- 0.4410 mL
- 2.2049 mL
- 4.4098 mL
- 10 mM
- 0.2205 mL
- 1.1024 mL
- 2.2049 mL

技术信息

CAS号

405554-55-4

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H27N5O2

运输

蓝冰

分子量

453.54

别名

溶解度

DMSO	10.0 mg/mL (22.0 mM) warming
Water	insoluble

动物实验配方

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靶点	Description	IC50
C-Raf		Ki:1.76nM
B-Raf		Ki:0.16nM

5-(2-(4-(2-(Dimethylamino)ethoxy)phenyl)-5-(pyridin-4-yl)-1H-imidazol-4-yl)-2,3-dihydro-1H-inden-1-one oxime Catalog No. CSN16576

靶点选择性

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