Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tesevatinib (XL-647) 是一种口服的多靶点酪氨酸激酶抑制剂,对 EGFR、ErbB2、KDR、Flt4和 EphB4的 IC50值分别为 0.3、16、1.5、8.7和 1.4 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 960 | 现货 | ||
2 mg | ¥ 1,170 | 现货 | ||
5 mg | ¥ 2,270 | 现货 | ||
10 mg | ¥ 3,950 | 现货 | ||
25 mg | ¥ 6,320 | 现货 | ||
50 mg | ¥ 8,670 | 现货 | ||
100 mg | ¥ 11,600 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,460 | 现货 |
产品描述 | Tesevatinib (XL-647) is an orally available, multi-target tyrosine kinase inhibitor (IC50s: 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4). |
靶点活性 | EGFR:0.3 nM, FLT4:8.7 nM, KDR:1.5 nM, ErbB2:16 nM |
体外活性 | Tesevatinib was inactive against a panel of 10 tyrosine kinases (including the insulin and the insulin-like growth factor-1 receptor) and 55 serine-threonine kinases (including cyclin-dependent kinases, stress-activated protein kinases, and protein kinase C isoforms). Tesevatinib inhibits cellular proliferation and EGFR pathway activation in the erlotinib-resistant H1975 cell line that harbors a double mutation (L858R and T790M) in the EGFR gene. In A431 cells, Tesevatinib reduces cell viability (IC50: 13 nM). |
细胞实验 | Growth inhibition of H1975 and A431 cells by increasing concentrations of Tesevatinib is determined by seeding 5000 cells per well in 96-well plates. The following day, cells are washed once with low-serum RPMI 1640 (0.1% fetal bovine serum, 1% nonessential amino acids, and 1% penicillin/streptomycin), after which 90 μL of the low-serum RPMI 1640 is added. Tesevatinib is diluted to 10 times the test concentrations and 10 μL are added to triplicate wells for a 72-h incubation. Cell viability is determined. |
动物实验 | Tumor-bearing mice are given either Tesevatinib, erlotinib, or gefitinib at 100 mg/kg and tumors are harvested 1 to 72 h later. Half an hour before the respective time point, EGF (50 μg/mouse) is given via i.v. bolus injection with tumors dissected 30 min later and tumor extracts are prepared by homogenization in 10 volumes of ice-cold lysis buffer. Lysates are clarified by centrifugation and EGFR tyrosine phosphorylation levels are determined by ELISA. |
别名 | KD-019, XL-647, EXEL-7647 |
分子量 | 491.39 |
分子式 | C24H25Cl2FN4O2 |
CAS No. | 781613-23-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30 mg/mL (61.05 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.035 mL | 10.1752 mL | 20.3504 mL | 50.8761 mL |
5 mM | 0.407 mL | 2.035 mL | 4.0701 mL | 10.1752 mL | |
10 mM | 0.2035 mL | 1.0175 mL | 2.035 mL | 5.0876 mL | |
20 mM | 0.1018 mL | 0.5088 mL | 1.0175 mL | 2.5438 mL | |
50 mM | 0.0407 mL | 0.2035 mL | 0.407 mL | 1.0175 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。
Tesevatinib 781613-23-8 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR VEGFR FLT Ephrin Receptor EXEL7647 HER1 XL647 Inhibitor KD-019 Vascular endothelial growth factor receptor XL-647 KD019 Epidermal growth factor receptor KD 019 EXEL-7647 ErbB-1 XL 647 EXEL 7647 inhibit inhibitor