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Rociletinib hydrobromide is an orally delivered inhibitor of the mutant form of EGFR kinase (Kis: 21.5 nM and 303.3 nM for EGFR L858R/T790M and EGFR WT).
Rociletinib hydrobromide is an orally delivered inhibitor of the mutant form of EGFR kinase (Kis: 21.5 nM and 303.3 nM for EGFR L858R/T790M and EGFR WT).
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
2 mg | ¥ 252 | 5日内发货 | |
5 mg | ¥ 413 | 5日内发货 | |
10 mg | ¥ 663 | 5日内发货 | |
25 mg | ¥ 1,130 | 5日内发货 | |
1 mL x 10 mM (in DMSO) | ¥ 578 | 5日内发货 |
产品描述 | Rociletinib hydrobromide is an orally delivered inhibitor of the mutant form of EGFR kinase (Kis: 21.5 nM and 303.3 nM for EGFR L858R/T790M and EGFR WT). |
靶点活性 | EGFR (T790M):303.3 nM (ki), EGFR (L858R/T790M):21.5 nM (ki) |
体外活性 | Rociletinib resistant NSCLC cell lines are sensitive to AKT inhibition. Rociletinib selectively inhibits the growth of NSCLC cells expressing mutant EGFR and induces apoptosis. Rociletinib (0.1 μM) inhibits EGFR potently and irreversibly. It inhibits more than 50% of 23 targets. |
体内活性 | Rociletinib (50 mg/kg bid, p.o.) shows anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice. Rociletinib (100 mg/kg/day, p.o.) displays anti-tumor activity in NSCLC EGFR mutant xenograft models. |
别名 | CO-1686 (hydrobromide), CNX-419 hydrobromide, AVL-301 hydrobromide |
分子量 | 636.46 |
分子式 | C27H29BrF3N7O3 |
CAS No. | 1446700-26-0 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 59 mg/mL (92.70 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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