Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability ofcancercells, and blocks tumor growth.

FAK^[1]

Y15 directly blocks autophosphorylation activity of FAK. Y15 inhibits Y397 phosphorylation of FAK starting at 0.1 μM in Panc-1 cells. At a dose of 100 μM, Y15 has the same or better inhibition as TAE226. Of note, total FAK is downregulated at higher doses of Y15. Y15 also blocks phosphorylation of the FAK downstream substrate, paxillin. Total paxillin is decreased at higher doses similar to FAK. Thus, Y15 inhibits FAK phosphorylation in a dose-dependent manner^[1]. MTS assay is completed using a range of Y15 doses on all cell lines (TT, K1, BCPAP, and TPC1, respectively).Y15 inhibited cell viability in a dose-dependent manner across all thyroid cell lines evaluated. IC₅₀is 2.05, 5.74, 9.99, and 17.54 μM for TT, TPC1, BCPAP, and K1, respectively^[2].
In macrophages treated with Y15, the filopodia and lamellipodia remain mobile. The lawn of particles surrounding macrophages appeared larger in cells treated with Y15^[4].

Nude mice bearing Panc si-ctrl xenografts are treated with TAE226, a dual FAK and IGF-1R tyrosine kinase inhibitor, to provide a reference for the antitumor effect of dual inhibition of FAK and IGF-1R. Without drug treatment, Panc si5-IGF-1R xenografts grew slower than Panc si-ctrl xenografts (Panc si5-IGF-1R/PBS vs. Panc si-ctrl/PBS), suggesting moderate tumor suppression by inhibiting the IGF-1R pathway only. Further inhibition of FAK activity by Y15 treatment suppresses the growth of Panc si5-IGF-1R xenografts more drastically (Panc si5-IGF-1R/PBS vs. Panc si5-IGF-1R/Y15). A similar antitumor effect is seen in Panc si-ctrl xenografts treated with TAE226 (Panc si5-IGF-1R/Y15 vs. Panc si-ctrl/TAE226). Mice demonstrates normal grooming and eating habits throughout the experiment^[3].

284.01

Solid

C₆H₁₄Cl₄N₄

4506-66-5

1,2,4,5-TETRAAMINOBENZENE 四盐酸盐

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

H₂O : 50 mg/mL(176.05 mM;ultrasonic and warming and heat to 50℃)

DMSO : 25 mg/mL(88.03 mM;ultrasonic and warming and heat to 60℃)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： PBS

  Solubility: 10 mg/mL (35.21 mM); Clear solution; Need ultrasonic and warming and heat to 60℃