PROTAC CDK12/13 Degrader-1 (7f) 是一种高效选择性的细胞周期蛋白依赖性激酶CDK12/CDK13双重降解剂，其DC50值分别是 2.2 nM 和 2.1 nM。PROTAC CDK12/13 Degrader-1 具有抗增殖活性，可用于乳腺癌的研究。

PROTAC CDK12/13 Degrader-1 (7f) 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 has anti-proliferative activity and can be used in breast cancer research [1].

PROTAC CDK12/13 Degrader-1 (7f) (0.02-10 μM, 150 h) significantly inhibits the proliferation of MFM223 and MDA-MB-231 cells in a dose-dependent manner [1]. PROTAC CDK12/13 Degrader-1 (7f) (500 nM, 4 h) can significantly degrade CDK12 and CDK13 of MFM223 and MDA-MB-231 cells in a dose-dependent manner [1]. Immunofluorescence [1] Cell Line: MDA-MB-231 cell lines Concentration: 1.0 μM Incubation Time: 15 hours Result: Showed 88% degradation for CDK12 and 74% for CDK13. Acted on CDK12 with the DC 50 value of 2.2 nM, and acted on CDK13 with the DC 50 value of 2.1 nM.

The pharmacokinetic parameters of PROTAC CDK12/13 Degrader-1 (7f) in rats [1]. Parameters oral (20 mg/kg) iv (10 mg/kg) ip (20mg/kg) iv (2.5 mg/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 max (ng/mL) 7.73 19892.4 24.79 1498.5 AUC 0-t (h*ng/mL) 21.83 7193.3 284.8 383.9 AUC 0-∞ (h*ng/mL) - 7242.7 318.5 391.55 CL (mL/h/kg) - 1406.5 - 6495.4 F (%) 0.15 - 10.63 -

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years