化合物CCT241161 T9638

Product Introduction
Bioactivity


英文名: CCT241161

描述: CCT241161 is an orally active pan-RAF inhibitor, with IC50 values of 3, 6, 10, 15, and 30 nM for LCK, CRAF, SRC, V600E-BRAF, and BRAF, respectively. It displays significant activity against BRAF and NRAS mutant melanomas, as well as demonstrating anticancer cell proliferative effects [1].

体外活性: CCT241161 (1, 3, 10, 30, 100 nM; 24 h) inhibits MEK and ERK in WM266.4 cells [1]. CCT241161 (1, 10, 100 nM and 1, 10, 100 μM) inhibits BRAF V600E in Ba/F3 cells [1]. CCT241161 (0.5 μM; 20 days) inhibits A375 cell without causing drug resistance [1]. CCT241161 (1 μM, 4 h) inhibits BRAF-inhibitor-resistant melanoma cells [1]. CCT241161 (0.1, 0.3, 1, 3, 10 μM; 24 h) inhibits MEK in NRAS mutant cells [1]. CCT241161 (0.1, 1, 10, 100 μM) shows anti-proliferative activity in D04 cells [1]. Cell Viability Assay [1] Cell Line: WM266.4 cells (BRAF mutant) Concentration: 1, 3, 10, 30, 100 nM Incubation Time: 24 h Result: Exhibited effects of inhibiting MEK and ERK in WM266.4 cells. Cell Viability Assay [1] Cell Line: Ba/F3 cells Concentration: 1, 10, 100 nM and 1, 10, 100 μM Incubation Time: Result: Inhibited BRAF-V600E and BRAF-T529N, V600E in Ba/F3 cells. Cell Viability Assay [1] Cell Line: A375 cell Concentration: 0.5 μM Incubation Time: 20 days Result: Maintained inhibitory activity against A375 cell,without drug resistance in 20 days. Cell Proliferation Assay [1] Cell Line: D04 cells Concentration: 0.1, 1, 10, 100 μM Incubation Time: Result: Efficiently inhibited NRAS mutant cell growth. Western Blot Analysis [1] Cell Line: patient #2 (PLX4720-resistant cells from patient with vemurafenib-resistant melanoma) Concentration: 1 μM Incubation Time: 4 h Result: Inhibited MEK, ERK, and SRC in the cells from patient #2. Western Blot Analysis [1] Cell Line: D04 cells Concentration: 0.1, 0.3, 1, 3, 10 μM Incubation Time: 24 h Result: Showed activity of surpressing MEK in NRAS mutant cells.

体内活性: CCT241161 (10, 20 mg/kg; i.g; once a day for 7 days) inhibits the growth of BRAF mutant A375, PLX4720-resistant A375 and NRAS mutant DO4 tumor xenografts in mice [1]. Animal Model: Female nude mice (5 to 6- week-old) [1]. Dosage: 10, 20 mg/kg Administration: Oral gavage; once a day for 7 days. Result: Showed activity of tumor regression in nude mice with xenografts tumor of BRAF mutant A375, PLX4720-resistant A375 (A375/R) and NRAS mutant DO4 without resulting in body weight loss to the mice.

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

溶解度: DMSO : Slightly soluble


关键字: CCT 241161 | CCT-241161 | CCT241161

相关产品: Raf inhibitor 1 dihydrochloride | Regorafénib N-oxyde (M2) | RAF265 | Uplarafenib | GW 5074 | B-Raf IN 15 | TAK-580 | Encorafenib | GDC-0879 | Sorafenib-d3

相关库: Anti-Cancer Compound Library | Bioactive Compounds Library Max | Anti-Ovarian Cancer Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Obesity Compound Library | Anti-Cancer Active Compound Library | Bioactive Compound Library

化合物CCT241161 T9638信息由TargetMol中国为您提供，如您想了解更多关于化合物CCT241161 T9638报价、型号、参数等信息，欢迎来电或留言咨询。

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