Y15

Y15 (1,2,4,5-Benzenetetramine tetrahydrochlor) 是一种特异性的粘着斑激酶抑制剂,能够降低其自身磷酸化活性,抑制癌细胞的活力,阻断肿瘤生长。

CAS号

4506-66-5

分子式

C6H14Cl4N4

主要靶点

FAK

仅限科研使用

Cat No : CM01156

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Synonyms

FAK inhibitor Y15|1,2,4,5-苯四胺四盐酸盐|1,2,4,5-Benzenetetramine tetrahydrochlor|FAK Inhibitor 14



产品信息

Y15 is a potent and specificsmall-molecule FAK scaffolding inhibitor that inhibits its autophosphorylation activity, blocks tumor growth.

CAS号 4506-66-5
分子式 C6H14Cl4N4
主要靶点 FAK
主要通路 蛋白酪氨酸激酶|细胞骨架|血管生成
分子量 284.01
纯度 98.00%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 FAK inhibitor Y15|1,2,4,5-苯四胺四盐酸盐|1,2,4,5-Benzenetetramine tetrahydrochlor|FAK Inhibitor 14

体外活性

Y15 inhibited viability in ?thyroid cancer cell lines in a dose-dependent manner[1].

溶解度

H2O:59 mg/mL (207.74 mM),Sonification/heating is recommended.

细胞实验

Apoptosis assay was done with PE Annexin V Apoptosis Detection Kit (BD) to identify apoptotic nuclei.?One hundred millimeter plates were seeded with TPC1, K1, BCPAP and TT cells at a concentration of 1 × 10^6 cells in normal growth media.?After overnight incubation, plates were treated with one of several doses of Y15 or left untreated.?After another 24 h of incubation, cells were collected with trypsin, and following centrifugation, were washed with 1× PBS.?Again, cells were centrifuged, PBS was removed and cells were resuspended in binding buffer and filtered through BD mesh tubes.?Annexin V and 7-AAD were added to the solution, vortexed and incubated for 15 minutes in the dark.?Binding buffer was added and the cells were analyzed by flow cytometry within 1 hour.

参考文献

1.O'Brien S, Golubovskaya VM, Conroy J,et al.FAK inhibition with small molecule inhibitor Y15 decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines and synergizes with targeted therapeutics[J].Oncotarget. 2014 Sep 15;5(17):7945-59.
2.Zheng D , Golubovskaya V , Kurenova E , et al. A novel strategy to inhibit FAK and IGF-1R decreases growth of pancreatic cancer xenografts[J]. Molecular Carcinogenesis, 2010, 49(2):0-0.
3.Hochwald S N , Nyberg C , Zheng M , et al. A novel small molecule inhibitor of FAK decreases growth of human pancreatic cancer[J]. Cell Cycle, 2009, 8(15):2435-2443.

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