货号	规格	价格	上海	北京	珠海	重庆	武汉
S83774-1mg	≥98%	￥416.00 S83774-1mg ￥416.00 3-5天	0 货期：3-5天	-	-	-	-
S83774-5mg	≥98%	￥885.00 S83774-5mg ￥885.00 3-5天	0 货期：3-5天	-	-	-	-
S83774-10mg	≥98%	￥1524.00 S83774-10mg ￥1524.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

FIIN-3 is an irreversible inhibitor of FGFR with an IC50 of 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.

靶点：

FGFR1:13.1 nM (IC50);FGFR2:21 nM (IC50);FGFR3:31.4 nM (IC50);FGFR4:35.3 nM (IC50);EGFR; FGFR

体外研究：

FIIN-3 potently inhibits both WT FGFRs (EC50 in the 1- to 41-nM range) and the gatekeeper mutant of FGFR2 (EC50 of 64 nM). FIIN-3 also strongly inhibits EGFR, with an EC50 of 43 nM. FIIN-3 shows good potency against gatekeeper mutant V564F; FIIN-3 also is potent against the gatekeeper-plus-1 mutant E565K; FIIN-3 also displays antiproliferative activity (with an EC50 of 135 nM) against Ba/F3 cells transformed by the EGFR vIII fusion protein, which has a WT EGFR kinase domain. FIIN-3 shows even better activity against EGFR mutant L858R (EC50 of 17 nM) and moderate activity, displaying an EC50 of 231 nM, against the EGFR mutant L858R/T790M mutant. In WT FGFR2 Ba/F3 cells, FIIN-3 completely inhibits the FGFR2 autophosphorylation on Tyr656/657 at concentrations as low as 3 nM. In FGFR2 V564M Ba/F3 cells, FIIN-3 is capable of inhibiting the FGFR2 mutant V564M autophosphorylation with partial inhibition at 100 nM and complete inhibition observed at 300 nM

参考文献：

1. Tan L et al. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc Natl Acad Sci U S A, 2014 Nov 11, 111(45):E4869-77

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.446 ml	7.23 ml	14.459 ml
5 mM	0.289 ml	1.446 ml	2.892 ml
10 mM	0.145 ml	0.723 ml	1.446 ml
50 mM	0.029 ml	0.145 ml	0.289 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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