DC Chemicals Limited
China
Product Name: Naquotinib mesylate
Price: $280.0/5mg $400.0/10mg $792.0/25mg
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: Naquotinib (mesylate)
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

1448237-05-5

1448237-05-5 structure

1448237-05-5 structure

Name: Naquotinib mesylate
Chemical Name: Naquotinib mesylate
CAS Number: 1448237-05-5
Molecular Formula: C₃₁H₄₆N₈O₆S
Molecular Weight: 658.812
Catalog: Research Areas Cancer
Create Date: 2018-04-04 06:51:56
Modify Date: 2024-01-03 14:12:37
Naquotinib mesylate (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.

Name	Naquotinib mesylate
Synonyms	6-Ethyl-3-{4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino}-5-{[(3R)-1-(prop-2-enoyl)pyrrolidin-3-yl]oxy}pyrazine-2-carboxamide monomethanesulfonate 6-ethyl-3-({4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5-{[(3R)-1-(1-oxoprop-2-en-1-yl)pyrrolidin-3-yl]oxy}pyrazine-2-carboxamide monomethanesulfonate UNII-12T09LV21O 5-{[(3R)-1-Acryloyl-3-pyrrolidinyl]oxy}-6-ethyl-3-({4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl}amino)-2-pyrazinecarboxamide methanesulfonate (1:1) ASP8273 mesilate Naquotinib mesilate Naquotinib mesylate 2-Pyrazinecarboxamide, 6-ethyl-3-[[4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-5-[[(3R)-1-(1-oxo-2-propen-1-yl)-3-pyrrolidinyl]oxy]-, methanesulfonate (1:1) 12T09LV21O Naquotinib (mesylate)

Description	Naquotinib mesylate (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
Related Catalog	Research Areas >> Cancer
Target	EGFRL858R/T790M EGFRL858R EGFRExon 19 deletion EGFRExon 19 deletion/T790M EGFR:230 nM (IC50)
In Vitro	In assays using endogenously EGFR-dependent cells, Naquotinib inhibits the growth of PC-9(del ex19), HCC827(del ex19), NCI-H1975(del ex19/T790M) and PC-9ER(del ex19/T790M) with IC50s of 8-33 nM[1]. Naquotinib selectively inhibits phosphorylation of EGFR and its down-stream signal pathway, ERK and Akt from 10nM in HCC827 and NCI-H1975 while inhibitory effects are only detected at 1000nM in A431.In NCI-H1650 (del ex19), Naquotinib inhibits cell growth with an IC50 value of 70nM while other EGFR-TKIs are only partially effective[2].
In Vivo	Oral Naquotinib treatment dose dependently induces tumor regression in NCI-H1975 (L858R/T790M), HCC827 (del ex19) and PC-9 (del ex19) xenograft models. Dosing schedules does not affect the efficacy of Naquotinib. In an NCI-H1975 xenograft model, complete regression of tumor is achieved after 14-days of Naquotinib treatment. Complete regression is maintained in 50% of mice more than 85 days after cessation of Naquotinib treatment[2].
References	[1]. Sakagami H, et al. ASP8273, a novel mutant-selective irreversible EGFR inhibitor, inhibits growth of non-small cell lung cancer (NSCLC) cells with EGFR activating and T790M resistance mutations. [abstract]. In: Proceedings of the 105th Annual Meeting of the American Association for Cancer Research; 2014 Apr 5-9; San Diego, CA. Philadelphia (PA): AACR; Cancer Res 2014;74(19 Suppl):Abstract nr 1728. doi:10.1158/1538-7445.AM2014-1728 [2]. Konagai S, et al. ASP8273 selectively inhibits mutant EGFR signal pathway and induces tumor shrinkage in EGFR mutated tumor models. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 2586. doi:10.1158/1538-7445.AM2015-2586

Molecular Formula	C₃₁H₄₆N₈O₆S
Molecular Weight	658.812
Exact Mass	658.326111
Storage condition	2-8℃