• 产品描述： 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[1][2]. Dalpiciclib shows antitumor activity against breast cancer and esophageal squamous cell carcinoma

• 靶点： CDK4:12.4 nM (IC50);CDK6:9.9 nM (IC50);CDK

• 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. Cell Proliferation Assay 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 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 IC50 values of 229.5, 115.4 and 210.7 nM, respectively.

• 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.

• 参考文献：
  1. Jose Manuel Perez-Garcia, et al. Perez-Garcia JM, Cortes J, Llombart-Cussac A. CDK4/6 inhibitors in breast cancer: spotting the difference. Nat Med. 2021 Nov;27(11):1868-1869. 2. Pin Zhang, et al. A phase 1 study of dalpiciclib, a cyclin-dependent kinase 4/6 inhibitor in Chinese patients with advanced breast cancer. Biomark Res. 2021 Apr 12;9(1):24. 3. Jiayuan Wang, et al. CDK4/6 inhibitor-SHR6390 exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated Rb and inducing G1 cell cycle arrest. J Transl Med. 2017 Jun 2;15(1):127. 4. Fei Long, et al. Preclinical characterization of SHR6390, a novel CDK 4/6 inhibitor, in vitro and in human tumor xenograft models. Cancer Sci. 2019 Apr;110(4):1420-1430.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.239 ml	11.197 ml	22.394 ml
  5 mM	0.448 ml	2.239 ml	4.479 ml
  10 mM	0.224 ml	1.12 ml	2.239 ml
  50 mM	0.045 ml	0.224 ml	0.448 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

输入产品批号：

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *