货号	规格	价格	上海	北京	珠海	重庆	武汉
S83375-1mg	≥98%	￥380.00 S83375-1mg ￥380.00 3-5天	0 货期：3-5天	-	-	-	-
S83375-5mg	≥98%	￥980.00 S83375-5mg ￥980.00 3-5天	0 货期：3-5天	-	-	-	-
S83375-10mg	≥98%	￥1680.00 S83375-10mg ￥1680.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR

靶点：

EGFRL858R/T790M;EGFRL858R;EGFRExon 19 deletion;EGFRExon 19 deletion/T790M;EGFR:230 nM (IC50);EGFR

体外研究：

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. 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

体内研究：

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

参考文献：

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. 2. Konagai S, et al. ASP8273 selectively inhibits mutant EGFR signal pathway and induces tumor shrinkage in EGFR mutated tumor models. 2015 Apr 18-22

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.518 ml	7.589 ml	15.179 ml
5 mM	0.304 ml	1.518 ml	3.036 ml
10 mM	0.152 ml	0.759 ml	1.518 ml
50 mM	0.03 ml	0.152 ml	0.304 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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Naquotinib (mesylate)