CR-1-31-B is a synthetic rocaglate and a potent eIF4A inhibitor. CR-1-31-B exhibits powerful inhibitory effects over eIF4A by perturbing the interaction between eIF4A and RNA, sequentially impeding initiation during protein synthesis. CR-1-31-B perturbs association of Plasmodium falciparum eIF4A (PfeIF4A) with RNA. CR-1-31-B induces apoptosis of neuroblastoma and gallbladder cancer cells.
性状
Solid
体外研究(In Vitro)
CR-1-31-B (100 nM; 24 hours) inhibits MUC1-C translation in MCF-10A cells (EGF-stimulated).CR-1-31-B (10 and 100 nM) decreases MUC1-C abundance in MDA-MB-468 breast cancer cells.CR-1-31B sensitizes gallbladder cancer cells to TRAIL-mediated apoptosis through the translational downregulation of c-FLIP.Neuroblastoma (NB) cell lines exhibit decreased viability, increased apoptosis rates as well as changes in cell cycle distribution when treated with the synthetic rocaglate CR-1-31-B (24-72 hours), which clamps eIF4A and eIF4F onto mRNA, resulting in a translational block.CR-1-31-B (100 nM; 5 hours) treatment increases reverse glutamine metabolism in pancreatic cancer cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
CR-1-31-B (2 mg/kg in 60 μL olive oil; IP; once every 2 days for 28 days) reduces the growth and initiates TRAIL-induced apoptosis in a BALB/c nude mice model of gallbladder cancer cells (GBC).
CR-1-31-B (0.2?mg/kg; IP; daily for 7 days; murine orthotopic transplant model of pancreatic ductal adenocarcinoma) effectively inhibits protein synthesis and growth of pancreatic tumours. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Jin C, Rajabi H, Rodrigo CM, Porco JA Jr, Kufe D. Targeting the eIF4A RNA helicase blocks translation of the MUC1-C oncoprotein. Oncogene. 2013;32(17):2179-2188.[2]. Cao Y, et al. Targeting eIF4A using rocaglate CR 1 31B sensitizes gallbladder cancer cells to TRAIL mediated apoptosis through the translational downregulation of c FLIP. Oncol Rep. 2021;45(1):230-238.
溶解度数据
In Vitro: DMSO : 230 mg/mL (453.18 mM; Need ultrasonic)配制储备液