4506-66-5
基本信息
FAK自磷酸化抑制剂(Y15
1,2,4,5-四氨基苯盐酸盐
1,2,4,5-苯四胺四盐酸盐
苯-1,2,4,5-四胺四盐酸盐
1,2,4,5-苯四胺四盐酸盐 5G
1,2,4,5-TETRAAMINOBENZENE 四盐酸盐
1,2,4,5-苯四胺四盐酸盐,1,2,4,5-BENZENETETRAAMINE TETRAHYDROCHLORIDE
1,2,4,5-苯四胺 四盐酸盐,1,2,4,5-BENZENETETRAMINE TETRAHYDROCHLORIDE
1,2,4,5-苯四胺四盐酸盐,1,2,4,5-BENZENETETRAAMINE TETRAHYDROCHLORIDE,1,2,4,5-苯四胺 四盐酸盐,1,2,4,5-BENZENETETRAMINE TETRAHYDROCHLORIDE
Y-15
NSC 667249
FAK Inhibitor 14
FAK inhibitor Y15
Benzene-1,2,4,5-tetrayL
tetraamine tetrahydrochL
Benzene-1,2,4,5-tetraMine 4HCl
1,2,4,5-Benzenetetraamine 4HCl
1,2,4,5-BenzenetetraminetetraHCl
物理化学性质
| 熔点 | ≥300 °C(lit.) |
| 熔点 | ≥300 °C(lit.) |
| 储存条件 | Desiccate at RT |
| 储存条件 | room temp |
| 溶解度 | 在水中的溶解度为20mg/mL，澄清 |
| 形态 | 粉末 |
| 颜色 | 淡紫色至深棕色 |
| BRN | 3701344 |
| 稳定性 | 可在-20°下的DMSO或蒸馏水中的溶液储存长达1个月。 |
| InChIKey | BZDGCIJWPWHAOF-UHFFFAOYSA-N |
安全数据
| 危险性符号(GHS) |   GHS02,GHS05 |
| 警示词 | 危险 |
| 危险性描述 | H225-H314 |
| 防范说明 | P210-P233-P240-P241-P242-P243-P260-P264-P280-P301+P330+P331-P303+P361+P353-P304+P340-P305+P351+P338-P310-P363-P370+P378-P403+P235-P405-P501 |
| 危险品标志 | Xi |
| 危险类别码 | 36/37/38 |
| 安全说明 | 26-36 |
| WGK Germany | 3 |
| WGK Germany | 3 |
| F | 10 |
常见问题列表
1,2,4,5-苯四胺四盐酸盐以剂量和时间依赖性方式直接阻断粘着斑激酶（FAK）的磷酸化，并且还显示出体内乳腺肿瘤消退。已经提出用FAK抑制剂14靶向FAK的Y397位点可以有效地用于癌症治疗。
| Target | Value |
|
FAK
(Cell-free assay) |
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. 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. IC 50 is 2.05, 5.74, 9.99, and 17.54 μM for TT, TPC1, BCPAP, and K1, respectively.
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.