Deltarasin trihydrochloride

产品名称：

1440898-61-2
Deltarasin trihydrochloride
2-[4-[(2S)-2-(2-Phenyl-1H-benzimidazol-1-yl)-2-(4-piperidinyl)ethoxy]phenyl]-1-(phenylmethyl)-1H-benzimidazole trihydrochloride
(S)-1-Benzyl-2-(4-(2-(2-phenyl-1H-benzo[d]imidazol-1-yl)-2-(piperidin-4-yl)ethoxy)phenyl)-1H-benzo[d]imidazole trihydrochloride

产品介绍：

产品说明

生化/生理作用

Deltarasin is a membrane-permeable benzimidazole derivative that effectively abolishes cellular KRas plasma membrane localization (5 μM for 1 hr) by blocking KRas-PDEδ interaction via high affinity interaction with PDEδ prenyl-binding pocket (K_D = 38 nM). Deltarasin inhibits oncogenic KRas-dependent proliferation (by ~50% of Panc-Tu-I cells; 5μM for 70 hrs) and survival (52% and 46% death induction of Panc-Tu-I and Capan-1 cells, respectively; 5μM for 24 hrs) in human pancreatic ductal adenocarcinoma (PDAC) cultures and is efficacious against Panc-Tu-I xenograft-derived tumor growth in mice in vivo (60% and 80% retardation on day 9, respectively, with 15 mg/kg q.d. or 10 mg/kg b.i.d. via i.p.).

基本信息

经验(实验)分子式	C₄₀H₃₇N₅O · 3HCl
分子量	713.14

产品性质

测定	≥98% (HPLC)
形式	powder
颜色	white to beige
溶解性	H₂O: 2 mg/mL, clear
储存温度	2-8℃

安全信息

储存分类代码	13 - Non Combustible Solids
WGK	WGK 3