Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 248 | 现货 | ||
2 mg | ¥ 355 | 现货 | ||
5 mg | ¥ 578 | 现货 | ||
10 mg | ¥ 995 | 现货 | ||
25 mg | ¥ 1,660 | 现货 | ||
50 mg | ¥ 2,470 | 现货 | ||
100 mg | ¥ 3,680 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 656 | 现货 |
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. |
靶点活性 | BRAF:0.1 μM, Raf:0.01 μM, Lck:0.02 μM, Src:0.03 μM, B-Raf (V600E):0.04 μM |
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 |
分子量 | 513.52 |
分子式 | C27H24FN7O3 |
CAS No. | 1163719-56-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: Insoluble
DMSO: 100 mg/mL (194.73 mM)
H2O: Insoluble
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9473 mL | 9.7367 mL | 19.4734 mL | 48.6836 mL |
5 mM | 0.3895 mL | 1.9473 mL | 3.8947 mL | 9.7367 mL | |
10 mM | 0.1947 mL | 0.9737 mL | 1.9473 mL | 4.8684 mL | |
20 mM | 0.0974 mL | 0.4868 mL | 0.9737 mL | 2.4342 mL | |
50 mM | 0.0389 mL | 0.1947 mL | 0.3895 mL | 0.9737 mL | |
100 mM | 0.0195 mL | 0.0974 mL | 0.1947 mL | 0.4868 mL |
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。
CCT196969 1163719-56-9 Angiogenesis MAPK Tyrosine Kinase/Adaptors Raf Src CCT 196969 Inhibitor inhibit CCT-196969 Raf kinases inhibitor