化合物CCT196969 T4133

Product Introduction
Bioactivity


英文名: CCT196969

描述: 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。

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

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: 口服CCT196969，每日10 mg/kg，24小时后可在血浆中测得约1 μM浓度。其口服生物利用度约为55%。在评估的剂量下，CCT196969极为安全耐受，且在体内不产生任何显著不良效应。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : Insoluble
DMSO : 100 mg/mL (194.73 mM)
H2O : Insoluble


关键字: Raf | CCT 196969 | CCT196969 | Inhibitor | inhibit | CCT-196969 | Raf kinases

相关产品: AD80 | Vemurafenib | Raf inhibitor 3 | Regorafenib | Pluripotin | Regorafenib Hydrochloride | Doramapimod | Pepinh-TRIF TFA | L-779450 | MRTX0902

相关库: Anti-Prostate Cancer Compound Library | Glutamine Metabolism Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Colorectal Cancer Compound Library | Tyrosine Kinase Inhibitor Library | Apoptosis Compound Library | Autophagy Compound Library | NO PAINS Compound Library | MAPK Inhibitor Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途