Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Olmutinib (HM61713, BI 1482694) 是可口服的不可逆 EGFR 酪氨酸激酶抑制剂,其与激酶结构域附近的半胱氨酸残基结合,可用于非小细胞肺癌的研究。
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 | ¥ 987 | 现货 | ||
25 mg | ¥ 1,830 | 现货 | ||
50 mg | ¥ 3,160 | 现货 | ||
100 mg | ¥ 4,320 | 现货 | ||
200 mg | ¥ 6,250 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 638 | 现货 |
产品描述 | Olmutinib (HM61713, BI 1482694) is an orally available small molecule, a mutant-selective inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Olmutinib binds to and inhibits mutant forms of EGFR, thereby leading to cell death of EGFR-expressing tumor cells. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced as compared to non-selective EGFR inhibitors which also inhibit the EGFR wild-type form. |
靶点活性 | BTK:13.9 nM |
体外活性 | HM61713 causes potent inhibition in cell lines H1975 (L858R and T790M) and HCC827 (exon 19 deletion). It has a low potency for NSCLC cell line H358 harboring wild-type EGFR (GI50 of 2225 nM)[1]. |
体内活性 | HM61713 has a half-life of over 24 h for EGFR inhibition. In the in vivo studies of xenograft models with grafts of H1975 and HCC827, HM61713 is active against the tumors without showing any side effects[1]. |
别名 | HM61713, BI 1482694, 奥莫替尼, BI 1482694, HM61713 |
分子量 | 486.59 |
分子式 | C26H26N6O2S |
CAS No. | 1353550-13-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 22 mg/mL (45.2 mM)
DMSO: 90 mg/mL (185 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.0551 mL | 10.2756 mL | 20.5512 mL | 51.378 mL |
5 mM | 0.411 mL | 2.0551 mL | 4.1102 mL | 10.2756 mL | |
10 mM | 0.2055 mL | 1.0276 mL | 2.0551 mL | 5.1378 mL | |
20 mM | 0.1028 mL | 0.5138 mL | 1.0276 mL | 2.5689 mL | |
DMSO | 50 mM | 0.0411 mL | 0.2055 mL | 0.411 mL | 1.0276 mL |
100 mM | 0.0206 mL | 0.1028 mL | 0.2055 mL | 0.5138 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。
Olmutinib 1353550-13-6 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR BTK 1802181-20-9 HM-61713 奥西替尼 ErbB-1 HM61713, BI 1482694 BI1482694 inhibit HM61713, BI1482694 BI-1482694 HER1 HM61713, BI-1482694 Epidermal growth factor receptor 奥莫替尼 T6918 Inhibitor HM 61713 BI 1482694 HM61713 inhibitor