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CCT196969
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。
CCT196969图片
CAS NO:1163719-56-9
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
50 mg电议
100 mg电议

产品介绍
CCT196969 是泛-Raf 抑制剂,抑制B-Raf、BRafV600E和CRaf,IC50分别为 0.1、0.04、和 0.01 μM。

产品描述

CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.

体外活性

CCT196969 induces caspase 3 and PARP cleavage, thus induces apoptosis. CCT196969 does not drive paradoxical pathway activation and inhibit MEK/ERK in BRAF and NRAS mutant melanoma. CCT196969 is active against melanoma and colorectal cancer cell lines that are mutant for BRAF, but not cancer cells that are wild-type for BRAF and NRAS.

体内活性

Oral dosing at 10 mg/kg/day of CCT196969 results in plasma concentrations ~1 μM at 24 hr. It is orally bioavailable at ~55%. CCT196969 is extremely well tolerated at the doses assessed and does not produce any significant adverse effects in vivo.

细胞实验

Cell lines: cell line derived from a vemurafenib-resistant melanoma. Method: The three cell lines derived from tumors displaying resistance to vemurafenib are incubated with DMSO (control),PLX4720,CCT196969,or CCT241161 (1 μM; 4 hr).Protein extracts are prepared in CLB1 lysis buffer,and samples are analyzed by Zeptosens RPPA(reverse phase protein arrays).

动物实验

Animal Models: CD-1 mice. Formulation: 5% DMSO,95% water. Dosages: 20 mg/kg . Administration: oral gavage

Cas No.

1163719-56-9

分子式

C27H24FN7O3

分子量

513.533

储存和溶解度

DMSO:100 mg/mL (194.73 mM)
H2O:Insoluble
Ethanol:Insoluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years