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。
| 生物活性 | Dalpiciclib (SHR-6390) hydrochloride is an orally active and highly selective inhibitor ofCDK4and 6withIC50values of 12.4 nM and 9.9 nM, respectively[1][2]. Dalpiciclib hydrochloride shows antitumor activity against breastcancerand esophageal squamous cell carcinoma[1][2][3][4]. |
| IC50& Target | CDK4 12.4 nM (IC50) | CDK6 9.9 nM (IC50) |
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体外研究
(In Vitro) | 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 IC50values of 229.5, 115.4 and 210.7 nM, respectively. |
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体内研究
(In Vivo) | 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. |
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| Clinical Trial | |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 5 mg/mL(10.35 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.0704 mL | 10.3518 mL | 20.7035 mL | | 5 mM | 0.4141 mL | 2.0704 mL | 4.1407 mL | | 10 mM | 0.2070 mL | 1.0352 mL | 2.0704 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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