Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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].
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,630 | 现货 | ||
5 mg | ¥ 3,990 | 现货 | ||
10 mg | ¥ 5,690 | 现货 | ||
25 mg | ¥ 8,730 | 现货 | ||
50 mg | ¥ 11,780 | 现货 | ||
100 mg | ¥ 15,800 | 现货 | ||
500 mg | ¥ 31,800 | 现货 |
产品描述 | 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. |
分子量 | 541.62 |
分子式 | C28H27N7O3S |
CAS No. | 1163719-91-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: Slightly soluble
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
CCT241161 1163719-91-2 MAPK Raf CCT 241161 CCT-241161 Inhibitor inhibitor inhibit