Bioactivity | PROTAC CDK12/13 Degrader-1 (7f) TFA is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 TFA has anti-proliferative activity and can be used in breast cancer research[1]. |
Invitro | PROTAC CDK12/13 Degrader-1 TFA (0.02-10 μM, 150 h) 显著并呈呈剂量依赖性抑制 MFM223 和 MDA-MB-231 细胞的增殖[1]。PROTAC CDK12/13 Degrader-1 TFA (500 nM, 4 h) 以剂量依赖性方式显著降解 MFM223 和 MDA-MB-231 细胞的 CDK12 和 CDK13[1]。 Immunofluorescence[1] Cell Line: |
In Vivo | The pharmacokinetic parameters of PROTAC CDK12/13 Degrader-1 (7f) TFA in rats[1]. Parameters |
Name | PROTAC CDK12/13 Degrader-1 TFA |
Formula | C47H47F3N10O8 |
Molar Mass | 936.93 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | -20°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
Reference | [1]. Jianzhang Yang, et al. Discovery of a Highly Potent and Selective Dual PROTAC Degrader of CDK12 and CDK13. J Med Chem. 2022 Aug 8. |