Dalpiciclib (SHR-6390) hydrochloride 是一种具有口服活性和高选择性的CDK4/6抑制剂，IC50值分别为 12.4 nM 和 9.9 nM。Dalpiciclib hydrochloride 对乳腺癌和食道鳞状细胞癌显示出抗肿瘤活性。

Dalpiciclib (SHR-6390) hydrochloride is an orally active and highly selective inhibitor of CDK4 and 6 with IC 50 values of 12.4 nM and 9.9 nM, respectively [1] [2]. Dalpiciclib hydrochloride shows antitumor activity against breast cancer and esophageal squamous cell carcinoma [1] [2] [3] [4].

Dalpiciclib hydrochloride (0-4 μM, 72 h) inhibits cell proliferation in a dose-dependent manner [3]. Dalpiciclib hydrochloride (0-10 μM, 6 d) inhibits the proliferation of retinoblastoma-positive tumor cell lines [4]. Cell Proliferation Assay [3] Cell Line: Eca 109, Eca 9706 and KYSE-510 ESCC cell lines Concentration: 0-4 μM Incubation Time: 72 hours Result: Inhibited cell proliferation in a dose-dependent manner, with Eca 109 being the relative sensitive one and Eca 9706 being the relative resistant one. Cell Viability Assay [4] Cell Line: MCF7, MCF7/TR, BT-474/T cell lines Concentration: 0-10 μM Incubation Time: 6 days Result: Inhibited MCF7/TR cells, parental MCF7 cells and BT-474/T resistant cells with the IC 50 values of 229.5, 115.4 and 210.7 nM, respectively.

Dalpiciclib hydrochloride (oral gavage; 150 mg/kg; once weekly; 3 weeks) shows antitumor activity against ESCC xenografts [3]. Dalpiciclib hydrochloride combined with Paclitaxel (PTX) or Cisplatin (CDDP) offer synergistic inhibitory effects in ESCC xenografts [3]. Dalpiciclib hydrochloride (oral gavage; 37.5 mg/kg, 75 mg/kg, 150 mg/kg; once daily; 30 days) shows antitumor activity in human xenograft models [4]. Animal Model: NOD/SCID mice (ESCC PDXs models) [3] Dosage: 150 mg/kg Administration: Oral gavage; 150 mg/kg; once weekly; 3 weeks Result: Suppressed the growth of tumor. Animal Model: 5-week-old female Balb/cA-nude mice subcutaneously inoculated MCF7/ARO, COLO 205 and U87MG [4] Dosage: 37.5 mg/kg, 75 mg/kg, 150 mg/kg Administration: Oral gavage; 37.5 mg/kg, 75 mg/kg, 150 mg/kg; once daily; 30 days Result: Caused regression of all tumor xenografts at the highest dose tested.

C25H31ClN6O2

483.01

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