货号	规格	价格	上海	北京	珠海	重庆	武汉
V45565-1mg	≥98%	￥1550.00 V45565-1mg ￥1550.00 3-5天	0 货期：3-5天	-	-	-	-
V45565-5mg	≥98%	￥3890.00 V45565-5mg ￥3890.00 3-5天	0 货期：3-5天	-	-	-	-
V45565-10mg	≥98%	￥6210.00 V45565-10mg ￥6210.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.

靶点：

EGFRL858R/T790M

体外研究：

EGFR-IN-1 TFA (30 mg/kg; p.o.; daily for 2 weeks) displays significant tumor growth inhibition with no observed loss in body weight.
EGFR-IN-1 TFA evaluates in a time course PD experiment upon oral dosing at 30 mg/kg. EGFR-IN-1 TFA shows a >50% inhibition of phosphorylation of EGFR for >12 h. EGFR-IN-1 TFA reaches maximal concentration of 0.10 μM at 2 h and systemic exposure (AUC0-inf.) is 0.33 μM. h.

体内研究：

EGFR-IN-1 TFA (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.

参考文献：

1. Wurz RP, et al. Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors. ACS Med Chem Lett. 2015 Jul 27;6(9):987-92.

保存条件：

2-8°C, 干燥

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.591 ml	7.954 ml	15.908 ml
5 mM	0.318 ml	1.591 ml	3.182 ml
10 mM	0.159 ml	0.795 ml	1.591 ml
50 mM	0.032 ml	0.159 ml	0.318 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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