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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。
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 | 库存 | 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 x 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在细胞系H1975(L858R和T790M)及HCC827(外显子19缺失)中显示出强效的抑制作用。对于携带野生型EGFR的非小细胞肺癌细胞系H358(GI50为2225 nM)[1],其抑制效力较低。 |
体内活性 | HM61713对EGFR抑制具有超过24小时的半衰期。在携带H1975和HCC827移植物的异种移植模型的体内研究中,HM61713对肿瘤具有活性,而且没有显示出任何副作用[1]。 |
别名 | 奥莫替尼, HM61713, BI 1482694, HM61713, BI 1482694 |
分子量 | 486.59 |
分子式 | C26H26N6O2S |
CAS No. | 1353550-13-6 |
Smiles | CN1CCN(CC1)c1ccc(Nc2nc(Oc3cccc(NC(=O)C=C)c3)c3sccc3n2)cc1 |
密度 | 1.336 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | Ethanol: 22 mg/mL (45.2 mM) DMSO: 90 mg/mL (185 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
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