DYRKs-IN-1 hydrochloride is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC 50 s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 hydrochloride has antitumor activity.
性状
Solid
IC50 & Target[1][2]
DYRK1A 5 nM (IC50) DYRK1B 8 nM (IC50
体外研究(In Vitro)
DYRKs-IN-1 hydrochloride (compound 30) increases the cellular potency against the human colon tumor cell line SW 620 with an EC50 of 27 nM. DYRKs-IN-1 hydrochloride (Example 183) is a potent DYRKs inhibitor. 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
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Anderson K, et al. Pyrido[2,3-d]pyrimidines: discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6610-5.[2]. Kevin Anderson, et al. Pyrido pyrimidines. US20120184542A1.
溶解度数据
In Vitro: DMSO : 20.83 mg/mL (33.35 mM; ultrasonic and warming and heat to 60°C)H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)配制储备液