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Y15

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Chemical Structure| 4506-66-5 同义名 : -
CAS号 : 4506-66-5
货号 : A191099
分子式 : C6H14Cl4N4
纯度 : 97%
分子量 : 284.014
MDL号 : MFCD00012970
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(88.02 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(176.05 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
描述 FAK (Focal adhesion kinase), a non-receptor tyrosine kinase, can regulate the cytoskeleton and act as a scaffolding and signaling protein for other adhesion molecules. The expression of FAK and its phosphorylation status show a strong correlation with the invasive phenotype of aggressive human tumors. Y15 is a selective FAK inhibitor[1]. Treatment with Y15 caused decrease of p-FAK-Y397 in TT thyroid cancer cells at concentration of 1μM and 3μM, as well as decrease of both p-FAK-Y397 and FAK expression in TPC1, K1 and BCPAP thyroid cancer cells dose-dependently at concentration ranging 5-50μM. The cell viability showed that Y15 was much potent than Defactinib on growth inhibition of the four thyroid cancer cell lines, with IC50 values of 2.05μM, 5.74μM, 9.99μM and 17.54μM for TT, TPC1, BCPAP and K1 cells. The function of Y15 on this four cells through inhibition of FAK may due to increased detachment and necrosis, as well as decreased clonogenicity. Meanwhile, the distinct gene changes induced by Y15 from Defactinib may partially contribute to its synergism with Defactinib in medullary thyroid TT cells[2].
作用机制 Y15 can be docked into the structural pocket of FAK containing Y397 site.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.52mL

0.70mL

0.35mL

17.61mL

3.52mL

1.76mL

35.21mL

7.04mL

3.52mL
参考文献

[1]Hochwald SN, Nyberg C, et al. A novel small molecule inhibitor of FAK decreases growth of human pancreatic cancer. Cell Cycle. 2009 Aug;8(15):2435-43. Epub 2009 Aug 1.

[2]O'Brien S, Golubovskaya VM, 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. Oncotarget. 2014 Sep 15;5(17):7945-59.

[3]Golubovskaya V, Curtin L, et al. In vivo toxicity, metabolism and pharmacokinetic properties of FAK inhibitor 14 or Y15 (1, 2, 4, 5-benzenetetramine tetrahydrochloride). Arch Toxicol. 2015;89(7):1095-101.