PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC 50 =62 nM) and CDK9 (DC 50 =33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC 50 =0.12 μM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with Cereblon ligand.
性状
Solid
IC50 & Target[1][2]
CDK2 62 nM (DC50) CDK9 33 nM (DC50
体外研究(In Vitro)
PROTAC CDK2/9 Degrader-1 (0.25-3 μM; 48 hours) induces cell cycle blockage at the G2/M phase.PROTAC CDK2/9 Degrader-1 (500 nM; 2-24 hours) down-regulates the Mcl-1 protein level in PC-3 cells.PROTAC CDK2/9 Degrader-1 effectively degrades CDK2/9 in cell lines MCF-7, HCT-116 and 22Rv1, which all have high CDK2/9 expression.PROTAC CDK2/9 Degrader-1 inhibits both CDK2 and CDK9, with IC50 as 7.42 nM and 14.50 nM, respectively. 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]. Zhou F, et al. Development of selective mono or dual PROTAC degrader probe of CDK isoforms. Eur J Med Chem. 2019 Dec 6;187:111952.
溶解度数据
In Vitro: DMSO : 55 mg/mL (67.42 mM; Need ultrasonic)配制储备液