Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CEP-40783 (RXDX-106) 是一种有口服活性的,高效的,选择性的 AXL (IC50:7 nM) 和 c-Met (IC50:12 nM) 抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 263 | 现货 | ||
5 mg | ¥ 612 | 现货 | ||
10 mg | ¥ 993 | 现货 | ||
25 mg | ¥ 2,320 | 现货 | ||
50 mg | ¥ 2,970 | 现货 | ||
100 mg | ¥ 4,480 | 现货 | ||
200 mg | ¥ 6,290 | 现货 |
产品描述 | CEP-40783 (RXDX-106) is an effective, specific and orally active AXL/c-Met inhibitor (IC50: 7/12 nM). It also inhibits MER and TYRO3 (IC50: 29/19 nM). |
靶点活性 | Tyro3:19 nM (Biochemical), Mer:29 nM (Biochemical), Axl:7 nM (Biochemical), c-Met:12 nM (Biochemical) |
体外活性 | In AXL-transfected 293 gT cells, CEP-40783 is 27-fold more active compared to the recombinant enzyme (IC50: 0.26 nM). In GTL-16 cells, CEP-40783 also has superior activity against c-Met (IC50: 6 nM). The enhanced inhibitory activity of CEP-40783 in cells is attributed to its extended residence time on both c-Met and AXL, similar with a Type II mechanism. CEP-40783 shows high kinome selectivity against 298 kinases with an S90 of 0.04 (fraction of kinases showing >90% inhibition at 1 μM)[1]. |
体内活性 | CEP-40783 showed dose- and time-dependent inhibition of AXL phosphorylation using NCI-H1299 NSCL xenografts with ~80% target inhibition at 0.3 mg/kg 6 h post dose and complete target inhibition to >90% inhibition at 1 mg/kg between 6-24 h, while a 10 mg/kg po dose resulted in complete AXL inhibition up to 48 h post dosing. In AXL/NIH3T3 xenografts, 0.3 mg/kg po resulted in complete tumor regressions. CEP-40783 was also efficacious in reducing spontaneous lymph node and pulmonary metastatic tumor burden in the MDA-MB-231-luc and 4T1-luc orthotopic breast cancer models, respectively, at 10 and 30 mg/kg po. PK/PD evaluation of the c-Met activity of CEP-40783 (10, 30, 55 mg/kg po qdX5d) showed significant to complete inhibition of c-Met phosphorylation in GTL-16 gastric carcinoma xenografts. Efficacy studies in GTL-16 xenografts demonstrated significant anti-tumor efficacy (tumor stasis and regressions) at 10 and 30 mg/kg po. In EBC-1 NSCL xenografts, administration of CEP-40783 (3, 10 and 30 mg/kg, po qd) resulted in dose-related efficacy, with tumor stasis at 3 mg/kg, tumor regressions and >96% TGI at 10 mg/kg. |
别名 | CEP 40783, RXDX-106 |
分子量 | 588.56 |
分子式 | C31H26F2N4O6 |
CAS No. | 1437321-24-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: Insoluble
Ethanol: 2 mg/mL
DMSO: 5.89 mg/mL (10 mM), Sonification is recommended
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.6991 mL | 8.4953 mL | 16.9906 mL | 42.4766 mL |
5 mM | 0.3398 mL | 1.6991 mL | 3.3981 mL | 8.4953 mL | |
10 mM | 0.1699 mL | 0.8495 mL | 1.6991 mL | 4.2477 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。
CEP-40783 1437321-24-8 Tyrosine Kinase/Adaptors c-Met/HGFR TAM Receptor Mer Inhibitor RXDX 106 CEP 40783 Tyro3 RXDX106 CEP40783 RXDX-106 inhibit Axl inhibitor