产品
编 号:F741253
分子式:C25H30N6O2
分子量:446.54
产品类型
结构图
CAS No: 1637781-04-4
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产品详情
生物活性:
Dalpiciclib (SHR-6390) is an orally active and highly selective inhibitor of CDK4 and 6 with IC50 values of 12.4?nM and 9.9?nM, respectively. Dalpiciclib shows antitumor activity against breast cancer and esophageal squamous cell carcinoma.
体内研究:
Dalpiciclib (oral gavage; 150 mg/kg; once weekly; 3 weeks) shows antitumor activity against ESCC xenografts.Dalpiciclib combined with Paclitaxel (PTX) or Cisplatin (CDDP) offer synergistic inhibitory effects in ESCC xenografts.Dalpiciclib (oral gavage; 37.5 mg/kg, 75 mg/kg, 150 mg/kg; once daily; 30 days) shows antitumor activity in human xenograft models .Animal Model:NOD/SCID mice (ESCC PDXs models)
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
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.
体外研究:
Dalpiciclib (0-4 μM, 72 h) inhibits cell proliferation in a dose-dependent manner.Dalpiciclib (0-10 μM, 6 d) inhibits the proliferation of retinoblastoma-positive tumor cell lines.