IMR-1A, a acid metabolite of IMR-1, is a Notch inhibitor with an IC 50 of 0.5 μM. IMR-1A has a 50-fold increase in potency with respect to IMR-1. IMR-1 can metabolize in vivo to IMR-1A.
性状
Solid
IC50 & Target[1][2]
IC50: 0.5 μM (Notch)
体内研究(In Vivo)
IMR-1A (2 mg/kg (i.v.) and 100 mg/kg (i.p)) exhibits low systematic plasma clearance (CL = 7 mL/min/kg) with terminal elimination half-life (T1/2) of 2.22 h following a single i.v. administration. The normal liver blood flow in mice is 90 mL/min/kg and the Vss (volume of distribution) is ~4-fold. Plasma concentrations is quantifiable up to 24 h with Tmax of 0.50 h after i.p. administration. 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]. Astudillo L et al. The Small Molecule IMR-1 Inhibits the Notch Transcriptional Activation Complex to Suppress Tumorigenesis. Cancer Res. 2016 Jun 15;76(12):3593-603.
溶解度数据
In Vitro: DMSO : 2 mg/mL (6.15 mM; Need ultrasonic)H2O : 1 mg/mL (3.07 mM; ultrasonic and warming and heat to 80°C)配制储备液