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Osimertinib dimesylate

Catalog No. T10433 CAS 2070014-82-1

Synonyms: 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).

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Osimertinib dimesylate Chemical Structure

Osimertinib dimesylate, CAS 2070014-82-1

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2 mg	5 days	$ 30.00
5 mg	5 days	$ 39.00
10 mg	5 days	$ 55.00

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Biological Description

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Storage & Solubility Information

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) 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].

Synonyms	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), Sonification and heating are recommended.

References and Literature

1. Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61. 2. Finlay MR, et al. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistancemutations that spares the wild type form of the receptor. J Med Chem. 2014 Oct 23;57(20):8249-67.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Osimertinib dimesylate 2070014-82-1 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR Osimertinib Dimesylate AZD 9291 Osimertinib Mereletinib Mereletinib (dimesylate) AZD-9291 (dimesylate) AZD9291 AZD-9291 inhibitor inhibit

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