AZD-9291; Mereletinib MedChemExpress (MCE)

Product Name	AZD9291
Synonyms	AZD9291 AZD-9291 Mereletinib Osimertinib Intermediate 4 Mereletinib mesylate(AZD9291) Pharmaceutical Chemical Anticancer Drug Azd-9291 for for Lung Cancer 1421373-65-0 N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide Synonyms AZD9291 AZD-9291 Mereletinib Osimertinib Intermediate 4 Mereletinib mesylate(AZD9291) Pharmaceutical Chemical Anticancer Drug Azd-9291 for for Lung Cancer 1421373-65-0 N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide
CAS	1421373-65-0
EINECS	629-848-5
Chemical Formula	C28H33N7O2
Molecular Weight	499.61
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Package	10 mM * 1 mL;5 mg;10 mg;50 mg;100 mg;200 mg;500 mg
Price	Email to quote
Descriptions	Osimertinib Osimertinib MedChemExpress (MCE) HY-15772 1421373-65-0 AZD-9291 Descriptions Osimertinib Osimertinib MedChemExpress (MCE) HY-15772 1421373-65-0 AZD-9291 Mereletinib 99.96% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Osimertinib (AZD9291) (0-10 μM 72 hours) dramatically inhibits cell proliferation with IC50s of 41, 26, 41, and 31 nM, respectively[2].?Osimertinib (0-10 μM 72 hours) inhibits cell proliferation (Ba/F3 cells harboring a T790M mutation, exon 19del+T790M, or L858R+T790M) with IC50s of 6, 7, and 74 nM, respectively[2].?Osimertinib (0-10 μM 72 hours) inhibits Ba/F3 cells harboring EGFR exon 20 insertion mutations (IC50 ranging from 16 to 701 nM for A763_Y764insFQEA (FQEA), Y764_V765insHH (HH), A767_V769dupASV (ASV), and D770_N771insNPG (NPG) cells)[2].?Osimertinib shows high levels of phenotype potency in both sensitizing-mutant (mean IC50 of 8 nM in PC-9) and T790M (mean IC50s of 11 and 40 nM in H1975 and PC-9VanR respectively) EGFR cell lines. Osimertinib has much less activity towards wild-type EGFR (mean IC50s of 650 and 461 nM in Calu3 and H2073 respectively)[1].?Osimertinib (0.1 μM 48 hours) induces apoptosis in Ba/F3 cells (apoptosis rates of 40.9% and 90% in EGFR exon 19del+T790M, EGFR L858R+T790M respectively) [2]. Osimertinib (0.1-25 mg/kg p.o. daily for 14 days) induces significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1]. EGFRL858R 12 nM (IC50, Enzyme assays) EGFRL858R/T790M 1 nM (IC50, Enzyme assays) \| \| \| \| \| \| \| \| \| \| [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. [Content Brief] [2]. Hirano T, et al. Pharmacological and Structural Characterizations of Naquotinib, a Novel Third-Generation EGFR Tyrosine Kinase Inhibitor, in EGFR-Mutated Non-Small Cell Lung Cancer. Mol Cancer Ther. 2018 Apr 17(4):740-750. [Content Brief]
Supplier Website	http://www.medchemexpress.com/AZD-9291.html
Last Update	2025-10-14 16:03:33

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