| 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) |
| 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： |
-80℃（运输条件：冰袋低温运输） |
| 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京