Dalpiciclib (SHR-6390) 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 对乳腺癌和食道鳞状细胞癌显示出抗肿瘤活性。
| 生物活性 | Dalpiciclib (SHR-6390) is an orally active and highly selective inhibitor ofCDK4and 6withIC50values of 12.4 nM and 9.9 nM, respectively[1][2]. Dalpiciclib shows antitumor activity against breastcancerand esophageal squamous cell carcinoma[1][2][3][4]. |
| IC50& Target[1] | CDK4 12.4 nM (IC50) | CDK6 9.9 nM (IC50) |
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体外研究
(In Vitro) | Dalpiciclib (0-4 μM, 72 h) inhibits cell proliferation in a dose-dependent manner[3].
Dalpiciclib (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 IC50values of 229.5, 115.4 and 210.7 nM, respectively. |
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体内研究
(In Vivo) | Dalpiciclib (oral gavage; 150 mg/kg; once weekly; 3 weeks) shows antitumor activity against ESCC xenografts[3].
Dalpiciclib combined with Paclitaxel (PTX) or Cisplatin (CDDP) offer synergistic inhibitory effects in ESCC xenografts[3].
Dalpiciclib (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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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