Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the K i values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively. In Vitro Rociletinib (0.1 μM) inhibits EGFR potently and irreversibly, and inhibits more than 50% of 23 targets. Rociletinib potently and selectively inhibits growth of NSCLC cells expressing mutant EGFR and induces apoptosis. Rociletinib resistant NSCLC cell lines are sensitive to AKT inhibition. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Rociletinib (100 mg/kg/day, p.o.) demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft models. Rociletinib (50 mg/kg bid, p.o.) demonstrates anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:EGFR L858R/T790M 21.5 nM (Ki) EGFR T790M 303.3 nM (Ki)
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Rociletinib hydrobromide
CAS number：1446700-26-0 molecular formula：C27H29BrF3N7O3
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| Chinese alias | 氢溴酸罗西替尼 | ||
| English alias | - | ||
| CAS number | 1446700-26-0 | molecular formula | C27H29BrF3N7O3 |
| molecular weight | 636.46 g/mol | Exact mass | ≥98% |
| PSA | 112.000 Ų | logp | - |
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