1,2,4,5-苯四胺四盐酸盐

用途应用生物活性靶点体外研究体内研究 1,2,4,5-苯四胺四盐酸盐试剂级价格

1,2,4,5-苯四胺四盐酸盐

CAS号:4506-66-5
英文名:1,2,4,5-BENZENETETRAMINE TETRAHYDROCHLORIDE
中文名:1,2,4,5-苯四胺四盐酸盐
CBNumber:CB4137959
分子式:C6H11ClN4
分子量:174.63
MOL File:4506-66-5.mol

1,2,4,5-苯四胺四盐酸盐化学性质

熔点 :≥300 °C(lit.)
储存条件 :room temp
溶解度 :H2O: soluble20mg/mL, clear
形态 :powder
颜色 :, faint purple to dark brown
BRN :3701344
稳定性 :Stable for 2 years from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 1 month.
InChIKey :BZDGCIJWPWHAOF-UHFFFAOYSA-N

安全信息

危险品标志 :Xi
危险类别码 :36/37/38
安全说明 :26-36
WGK Germany :3
F :10

1,2,4,5-苯四胺四盐酸盐性质、用途与生产工艺

用途
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。
应用 1,2,4,5-苯四胺四盐酸盐淡紫色粉末，用于合成材料中间体和医药研发的中间体，可用于实验室研发和化工医药合成过程中。
生物活性 Y15是一种有效，特异性的粘着斑激酶抑制剂 (FAK)，可抑制其自身磷酸化活性，降低癌细胞的活力，阻断肿瘤生长。
靶点
Target Value
FAK
(Cell-free assay)
体外研究

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.
体内研究

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.