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Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $30 | 5 days | |
5 mg | $39 | 5 days | |
10 mg | $55 | 5 days |
Description | Osimertinib dimesylate is an irreversible and mutant selective EGFR inhibitor (IC50s: 12 and 1 nM against EGFR L858R and EGFR L858R/T790M). |
In vitro | Osimertinib (AZD-9291) shows similar potency to early generation tyrosine kinase inhibitor in inhibiting EGFR phosphorylation in EGFR cells harboring sensitizing EGFR mutants including PC-9 (ex19del), H3255 (L858R) and H1650 (ex19del) (mean IC50s: 13 to 54 nM). Osimertinib also potently inhibits phosphorylation of EGFR in T790M mutant cell lines H1975 (L858R/T790M), PC-9VanR (ex19del/T790M), with mean IC50 potency less than 15 nM [1]. |
In vivo | The tumor-bearing mice are treated with Osimertinib (5 mg/kg/day) for one to two weeks. Within days of treatment, 5 of 5 C/L858R mice display nearly 80% reduction in tumor volume by magnetic resonance imaging MRI after therapy with Osimertinib, while 5 of 5 mice treated with vehicle shows tumor growth [1]. Upon dosing Osimertinib in three efficacy models, comparable efficacy is observed at relatively low doses (10 mg/kg per day). The excellent efficacy is also observed when Osimertinib is dosed at 5 mg/kg per day [2]. |
Alias | Mereletinib (dimesylate), AZD-9291 (dimesylate) |
Molecular Weight | 691.82 |
Formula | C30H41N7O8S2 |
Cas No. | 2070014-82-1 |
Storage | keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||
Solubility Information | DMSO: 0.4 mg/mL (0.58 mM) | |||||
Solution Preparation Table | ||||||
DMSO
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