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Nazartinib mesylate

Catalog No. T11156L CAS 1508250-72-3

Synonyms: EGF816 (mesylate)

Nazartinib mesylate is a novel, covalent mutant-selective inhibitor of EGFR (Ki and Kinact: 31 nM and 0.222/min on EGFR(L858R/790M) mutant).

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Nazartinib mesylate, CAS 1508250-72-3

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

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Description	Nazartinib mesylate is a novel, covalent mutant-selective inhibitor of EGFR (Ki and Kinact: 31 nM and 0.222/min on EGFR(L858R/790M) mutant).
Targets&IC50	EGFR (L858R/T790M):31 nM （ki）
In vitro	Nazartinib inhibits cell proliferation (EC50: 9, 11, and 25 nM in H3255, HCC827, and H1975, respectively). Nazartinib has an inhibitory effect on the mutant cell lines (IC50s: 4, 6, 2 nM in H1975, H3255, and HCC827, respectively). It also shows improved ADME and PK properties [1]. Nazartinib has an OC50 value of 2 and 5 nM on HCC827 and H1975, respectively. Nazartinib displays potent inhibition of pEGFR levels in H3255, HCC827, and H1975 cell lines ( EC50: 5, 1, and 3 nM, respectively) [2].
In vivo	Nazartinib (50 and 20 mg/kg or 25 mg/kg, p.o.) demonstrates dose-dependent efficacy with near-complete tumor cells regression at the highest dose tested (50 mg/kg), in H1975 mouse xenograft model [1]. Nazartinib (30 mg/kg, p.o.) displays significant antitumor activity, in the H3255 xenograft model. In the H1975 mouse model, Nazartinib (10 mg/kg, p.o.) induces tumor growth inhibition with a T/C (tumor/control volume) of 29%, and when doses are 30 and 100 mg/kg, tumor regressions are achieved (T/C, ?61% and ?80%, respectively). Antiproliferative activity of Nazartinib on 89 lung cancer cell lines indicates that Nazartinib selectively inhibits cell lines containing EGFR with catalytic domain mutations [2].

Synonyms	EGF816 (mesylate)
Molecular Weight	591.12
Formula	C27H35ClN6O5S
CAS No.	1508250-72-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Lelais G, et al. Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T79 2. Jia Y, et al. EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor. Cancer Res. 2016 Mar 15;76(6):1591-602

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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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

Nazartinib mesylate 1508250-72-3 Others EGF 816 EGF816 (mesylate) EGF-816 EGF816 Nazartinib Mesylate inhibitor inhibit

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