货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V53148-1ml	10mM in DMSO	￥940.00 V53148-1ml ￥940.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V53148-1ml

10mM in DMSO

￥940.00

货期：3-5天

产品描述：

CEP-37440 is a potent, orally active dual FAK/ALK inhibitor with IC50 values of 2.3 nM and 3.5 nM for FAK and ALK, respectively. CEP-37440 decreases the cell proliferation by blocking the autophosphorylation kinase activity of FAK1 (Tyr 397)

靶点：

IC50:2.3 nM (FAK) and 3.5 nM (ALK);FAK; ALK

体外研究：

CEP-37440 (0-3000 nM; 0-192 h) decreases the proliferation of inflammatory breast cancer (IBC) cells in a dose-dependent manner. CEP-37440 (1000 nM; 0-120 h) decreases phospho-FAK1 (Tyr 397) and maintains its low level over time in FC-IBC02, SUM 190, and KPL4. CEP-37440 (0-3000 nM; Sup-M2 and Karpas-299 cells) induces proapoptotic caspases in a dose-dependent manner. Cell Viability Assay Cell Line: FC-IBC02, KPL4, SUM190, MDA-IBC03 and SUM149 cells Concentration: 0, 300, 1000, 2000 and 3000 nM Incubation Time: 0, 24, 48, 72, 96, 120, 144, 168, and 192 hours Result: Reduced the proliferation of three out of five IBC cell lines at low concentration. Inhibited the proliferation almost completely at 3000 nM concentration. Western Blot Analysis Cell Line: FC-IBC02, SUM 190, and KPL4 cells Concentration: 1000 nM Incubation Time: 0, 48, 72, 96 and 120 hours Result: Decreased phospho-FAK1 by half in FC-IBC02, SUM190, and KPL4 cells after 48 hours.

体内研究：

CEP-37440 (3-55 mg/kg; p.o.; b.i.d and q.d., for 12 d) inhibits breast tumor growth in Sup-M2 xenograftin SCID mice. CEP-37440 (30 mg/kg; p.o; once, for 24 h) inhibits tyrosine phosphorylation in Sup-M2 xenografts mice. CEP-37440 (55 mg/kg; p.o; once, for 24 h) inhibits FAK phosphorylation in CWR22 xenografts in Nude mice. CEP-37440 (1-10 mg/kg; p.o and i.v.; CD-1 mouse, Sprague-Dawley (SD) rats) has good pharmacokinetic parameters. Animal Model: SCID/Beige with Sup-M2 xenografts Dosage: 3 mg/kg (b.i.d), 10 mg/kg (b.i.d), 30 mg/kg (b.i.d and q.d. ), and 55 mg/kg (q.d.) Administration: Oral administration; b.i.d and q.d., for 12 days Result: Inhibited tumor growth in a dose-dependent manner.

溶解性：

Soluble in DMSO、H2O

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.724 ml	8.619 ml	17.238 ml
5 mM	0.345 ml	1.724 ml	3.448 ml
10 mM	0.172 ml	0.862 ml	1.724 ml
50 mM	0.034 ml	0.172 ml	0.345 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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