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PROTAC CDK12/13 Degrader-1 (7f) TFA is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC 50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 TFA has anti-proliferative activity and can be use
Appearance:Solid
IC50& Target:CDK12 2.2 nM (DC 50 ) CDK13 2.1 nM (DC 50 )
In Vitro:PROTAC CDK12/13 Degrader-1 (7f) TFA (0.02-10 μM, 150 h) significantly inhibits the proliferation of MFM223 and MDA-MB-231 cells in a dose-dependent manner. PROTAC CDK12/13 Degrader-1 (7f) TFA (500 nM, 4 h) can significantly degrade CDK12 and CDK13 of
In Vivo:The pharmacokinetic parameters of PROTAC CDK12/13 Degrader-1 (7f) TFA in rats. Parameters oral (20mg/kg) iv (10mg/kg) ip (20mg/kg) iv (2.5mg/kg) t 1/2 (h) - 5.28 10.85 5.8 T max (h) 5.33 0.08 2.17 0.08 C max (ng/mL) 7.73 19892.4 24.79 1498.5 C ma
Biological Activity:PROTAC CDK12/13 Degrader-1 (7f) TFA is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC 50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 TFA has anti-proliferative activity and can be use