YX-2-107 (10 mg/kg; i.p.; single) 显示最大浓度为 741 nM (比 CDK6 降解 IC50 高 150 倍),4 小时后从血浆中清除。 YX-2-107 (150 mg/kg; i.p.; single daily for 3 days) 在抑制大鼠体内 Ph+ ALL 增殖中具有药理学活性。
参考文献:
1. De Dominici M, et al. Selective inhibition of Ph-positive ALL cell growth through kinase-dependent and -independent effects by CDK6-specific PROTACs. Blood. 2020 Apr 30;135(18):1560-1573.