中文名 | 罗加替尼 |
英文名 | BAY-1163877 |
别名 | 罗加替尼 化合物ROGARATINIB 成纤维细胞生长因子受体(FGFR)抑制剂(ROGARATINIB) 4-{[4-氨基-6-(甲氧基甲基)-5-(7-甲氧基-5-甲基-1-苯并噻吩-2-基)吡咯[2,1-F]-[1,2,4]三嗪-7-基]甲基}哌嗪-2-酮 |
英文别名 | BAY-1163877 Rogaratinib Rogaratinib (BAY1163877) 2-Piperazinone, 4-[[4-amino-6-(methoxymethyl)-5-(7-methoxy-5-methylbenzo[b]thien-2-yl)pyrrolo[2,1-f][1,2,4]triazin-7-yl]methyl]- 4-{[4-amino-6-(methoxymethyl)-5-(7-methoxy-5-methyl-1-benzothiophen-2-yl)pyrrolo[2,1-f]-[1,2,4]triazin-7-yl]methyl}piperazin-2-one |
CAS | 1443530-05-9 |
化学式 | C23H26N6O3S |
分子量 | 466.56 |
密度 | 1.48±0.1 g/cm3(Predicted) |
溶解度 | DMSO :2 mg/ml (需要超声波) |
酸度系数 | 15.49±0.20(Predicted) |
存储条件 | -20°C |
产品用途 | Rogaratinib, also known as BAY-1163877, is an aberrant fibroblast growth factor receptor (FGFR) inhibitor. Rogaratinib is as an orally available, selective and potent inhibitor of FGFR-1, -2 and -3 kinase activity. FGFRs are a family of receptor tyrosine kinases, which may be upregulated in various tumor cell types and may be involved in tumor cell differentiation and proliferation, tumor angiogenesis, and tumor cell survival. |
靶点 | FGFR |
上游原料 | 7-METHOXY-5-METHYLBENZO[B]THIOPHENE 7-甲氧基-5-甲基-苯并噻砜-2-硼酸 2-哌嗪酮 2-甲氧基-4-甲基苯胺 (2,2-diethoxyethyl)(2-methoxy-4-methylphenyl)sulfane 2-甲氧基-4-甲基苯磺酰氯 5-甲基-2-硝基茴香醚 |
参考资料 展开查看 | 1. Sylvia Grünewald , Oliver Politz , Sebastian Bender,et al.Rogaratinib: A potent and selective pan-FGFR inhibitor with broad antitumor activity in FGFR-overexpressing preclinical cancer models.Int J Cancer. 2019 Sep 1;145(5):1346-1357.2. Kim SM, et al. Activation of the Met kinase confers acquired drug resistance in FGFR-targeted lung cancer therapy. Oncogenesis. 2016 Jul 18;5(7):e241. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.143 ml | 10.717 ml | 21.433 ml |
5 mM | 0.429 ml | 2.143 ml | 4.287 ml |
10 mM | 0.214 ml | 1.072 ml | 2.143 ml |
5 mM | 0.043 ml | 0.214 ml | 0.429 ml |
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