1,2,4,5-苯四胺四盐酸盐
中文名称:
1,2,4,5-苯四胺四盐酸盐
中文同义词:
1,2,4,5-苯四胺四盐酸盐;1,2,4,5-苯四胺;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-TETRAAMINOBENZENE 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,1,2,4,5-BENZENETETRAMINE TETRAHYDROCHLORIDE;FAK自磷酸化抑制剂(Y15;1,2,4,5-苯四胺四盐酸盐,1,2,4,5-BENZENETETRAAMINE TETRAHYDROCHLORIDE
英文名称:
1,2,4,5-BENZENETETRAMINE TETRAHYDROCHLORIDE
英文同义词:
1,2,4,5-TETRAAMINOBENZENE TETRAHYDROCHLORIDE;1,2,4,5-BENZENETETRAMINE TETRAHYDROCHLORIDE;1,2,4,5-Benzenetetraamine tetrahydrochloride;benzene-1,2,4,5-tetrayltetraamine tetrahydrochloride;1,2,4,5-BENZENETETRAMINE TETRAHYDRO-CHLO RIDE, TECH.;1,2,4,5-BenzenetetraminetetraHCl;1,2,4,5-Benzenetetramine tetrahydrochloride, 1,2,4,5-Tetraaminobenzene tetrahydrochloride;(2,4,5-triaminophenyl)amine tetrahydrochloride
CAS号:
4506-66-5
分子式:
C6H11ClN4
分子量:
174.63
EINECS号:
224-822-6
相关类别:
含硫化合物;细胞生物学试剂;有机化学;Selective focal adhesion kinase (FAK) inhibitor that displays no significant activity at a range of other kinases including EGFR, PDGFR and IGF-RI.
Mol文件:
4506-66-5.mol
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
InChIKey
BZDGCIJWPWHAOF-UHFFFAOYSA-N
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)
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.
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
