Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC 50 s of 12 and 1 nM against EGFR L858R and EGFR L858R/T790M , respectively. In Vitro Osimertinib (AZD-9291) shows similar potency to early generation tyrosine kinase inhibitor (TKIs) in inhibiting EGFR phosphorylation in EGFR cells harboring sensitising EGFR mutants including PC-9 (ex19del), H3255 (L858R) and H1650 (ex19del), with mean IC 50 values ranging from 13 to 54 nM for Osimertinib (AZD-9291). Osimertinib (AZD-9291) also potently inhibits phosphorylation of EGFR in T790M mutant cell lines (H1975 (L858R/T790M), PC-9VanR (ex19del/T790M), with mean IC 50 potency less than 15 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo The tumor-bearing mice are treated with Osimertinib (AZD-9291) (5 mg/kg/day) for one to two weeks. Within days of treatment, 5 of 5 C/L858R mice displays nearly 80% reduction in tumor volume by magnetic resonance imaging MRI after therapy with Osimertinib (AZD-9291), while 5 of 5 mice treated with vehicle shows tumor growth . Osimertinib (AZD-9291) demonstrates improved rat PK, reduced hERG affinity, and improved IGF1R margins relative to the previously described compounds, and so this compound is selected for further investigation. Osimertinib (AZD-9291) also offers an additional degree of broader chemical and profile diversity when compared to the previously described lead compounds. Upon dosing Osimertinib (AZD-9291) in three efficacy models, The comparable efficacy is observed at relatively low doses (10 mg/kg per day). The excellent efficacy is also observed when Osimertinib (AZD-9291) is dosed at 5 mg/kg per day. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:EGFR L858R 12 nM (IC 50 ) EGFR L858R/T790M 1 nM (IC 50 )
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Osimertinib dimesylate
CAS number：2070014-82-1 molecular formula：C30H41N7O8S2
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| Chinese alias | 奥希替尼二甲磺酸盐 | ||
| English alias | - | ||
| CAS number | 2070014-82-1 | molecular formula | C30H41N7O8S2 |
| molecular weight | 691.82 g/mol | Exact mass | ≥98% |
| PSA | - | logp | - |
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