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Osimertinib dimesylate
Catalog No. T10433Cas No. 2070014-82-1
Alias Mereletinib (dimesylate), AZD-9291 (dimesylate)
Osimertinib dimesylate is an irreversible and mutant selective EGFR inhibitor (IC50s: 12 and 1 nM against EGFR L858R and EGFR L858R/T790M).
Osimertinib dimesylate
Catalog No. T10433Alias Mereletinib (dimesylate), AZD-9291 (dimesylate)Cas No. 2070014-82-1
Osimertinib dimesylate is an irreversible and mutant selective EGFR inhibitor (IC50s: 12 and 1 nM against EGFR L858R and EGFR L858R/T790M).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $30 | 5 days | |
| 5 mg | $39 | 5 days | |
| 10 mg | $55 | 5 days |
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Osimertinib dimesylate is an irreversible and mutant selective EGFR inhibitor (IC50s: 12 and 1 nM against EGFR L858R and EGFR L858R/T790M). |
| Targets&IC50 | EGFR (L858R/T790M):1 nM, EGFR (L858R):12 nM |
| In vitro | Osimertinib (AZD-9291) exhibits similar potency to early-generation tyrosine kinase inhibitors in inhibiting EGFR phosphorylation in EGFR cells with sensitizing EGFR mutations, including PC-9 (ex19del), H3255 (L858R), and H1650 (ex19del) (mean IC50s: 13-54 nM). Additionally, Osimertinib potently inhibits EGFR phosphorylation in T790M mutant cell lines H1975 (L858R/T790M) and PC-9VanR (ex19del/T790M), with mean IC50s below 15 nM [1]. |
| In vivo | Tumor-bearing mice are treated with Osimertinib (5 mg/kg/day) for one to two weeks. Within days of treatment, 5 out of 5 C/L858R mice exhibit nearly 80% reduction in tumor volume by MRI, while 5 out of 5 vehicle-treated mice show tumor growth [1]. Comparable efficacy is observed at low doses (10 mg/kg per day) in three efficacy models, and excellent efficacy is also noted 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 & Solubility Information
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO: 0.4 mg/mL (0.58 mM), Sonication and heating are recommended. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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