IV-361 is an orally active and selective CDK7 inhibitor (K i ≤50 nM). IV-361 has anti-cancer activity (US20190256531A1).
性状
Solid
IC50 & Target[1][2]
CDK7 ≤50 nM (Ki) CDK2 ≥1000 nM (Ki)
体外研究(In Vitro)
IV-361 has less inhibition on CDK2 (Ki≥1000 nM) or PLK1 (Ki≥5000 nM). IV-361 exhibits excellent IL-2 and IL-17 production inhibitory activity (all IC50≤100 nM) in periphery blood mononuclear cell (PBMC). IV-361 exhibits excellent HCT-116 cell growth inhibitory activity (GI50≤100 nM). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
IV-361 (25 mg/kg/day; orally) exhibits 46% or more rate of suppression of tumor volume in female BALB nude mice with HCT-116. 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]. Noriaki Iwase, et al. Substituted dihydropyrrolopyrazole derivative. US20190256531A1.
溶解度数据
In Vitro: DMSO : 90 mg/mL (196.67 mM; Need ultrasonic)配制储备液