Dalpiciclib 是一种高选择性、口服生物利用度和相当效力的 CDK4 和 CKD6 抑制剂，IC50 分别为 12.4?nM 和 9.9?nM。它通过抑制磷酸化 Rb 蛋白和诱导 G1 细胞周期阻滞在食管鳞状细胞癌中发挥有效的抗肿瘤活性。

Dalpiciclib is a highly selective, orally bioavailable, and comparable potency inhibitor of CDK4 and CKD6 with IC50s of 12.4 nM and 9.9 nM, respectively. Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest.

Dalpiciclib inhibits cell proliferation in a dose-dependent manner following administration of 0-4 μM for 72?hours[2].In the relative sensitive Eca 109 and KYSE-510 cell lines, Dalpiciclib significantly blocks Rb phosphorylation at serine 780 after 24 hours of administration and induces cell cycle arrest but not in relative resistant Eca 9706 cell line[2].

Dalpiciclib administered at 150 mg/kg weekly for 3 weeks by oral gavage has antitumor activity in ESCC xenografts[2]. Dalpiciclib in combination with Paclitaxel or Cisplatin provides synergistic inhibition in ESCC xenografts[2].

1637781-04-4

C25H30N6O2

446.54

SHR-6390

DMSO:3.5 mg/mL (7.84 mM),ultrasonic, adjust pH to 5 with HCl and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years