Riviciclib hydrochloride (P276-00) 是有效的CDK抑制剂，抑制CDK9-cyclinT1，CDK4-cyclin D1，CDK1-cyclinB的IC50值分别为 20 nM，63 nM，79 nM。Riviciclib hydrochloride (P276-00) 对 Cisplatin 耐药性细胞具有抗肿瘤活性。
| 生物活性 | Riviciclib hydrochloride (P276-00) is a potentcyclin-dependent kinase(CDK)inhibitor, which inhibitsCDK9-cyclinT1,CDK4-cyclin D1, andCDK1-cyclinBwithIC50s of 20 nM, 63 nM, and 79 nM, respectively[1][2].
Riviciclib hydrochloride (P276-00) shows antitumor activity on cisplatin-resistant cells[3]. |
| IC50& Target[1] | CDK9- Cyclin T1 0.020 μM (IC50) | cdk4-cyclin D1 0.063 μM (IC50) | CDK1-Cyclin B 0.079 μM (IC50) | cdk2-cyclin A 0.224 μM (IC50) | cdk2-cyclin E 2.500 μM (IC50) | cdk6-cyclin D3 0.396 μM (IC50) | CDK9-cyclin H 2.900 μM (IC50) |
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体外研究
(In Vitro) | Riviciclib hydrochloride (1.5-5 μM; 72 hours) shows no detectable cells in G1 and G2 in promyelocytic leukemia cells and arrest of cells in G1 in synchronized human non-small cell lung carcinoma (H-460) and human normal lung fibroblast (WI-38) cells[3].
Riviciclib hydrochloride (3-24 hours; 1.5 μM) reduces cyclin D1, Cdk4, and Rb levels in H-460 cells. Rb (retinoblastoma) phosphorylation at Ser780decrease at 3 h[2].
Riviciclib hydrochloride shows activity in human cancer cell lines, such as colon carcinoma, osteosarcomal, cervical carcinoma, and bladder carcinoma cells[2].
Cell Cycle Analysis[3] | Cell Line: | Promyelocytic leukemia cells (HL-60 cells), non-small cell carcinoma (H-460) cells, human normal lung fibroblast (WI-38) cells | | Concentration: | 1.5, 5 μM | | Incubation Time: | 72 hours | | Result: | Showed apoptosis at the end of 24 h and no detectable cells were present in G1 and G2 in HL-60 cells. Caused an exclusive G1 arrest of synchronous population of cancerous cells H-460 cells and normal cells WI-38. |
Western Blot Analysis[2] | Cell Line: | H-460 cells; MCF-7 cells | | Concentration: | 1.5 μM | | Incubation Time: | 3, 6, 9, 12, 24 hours | | Result: | Reduced cyclin D1, Cdk4, and Rb levels in H-460 cells. Rb (retinoblastoma) phosphorylation at Ser780decrease at 3 h. Decreased protein levels of cyclin D1 and Cdk4 levels staring at 6 and 9 h in MCF-7 cells, respectively, and accompanied by a decrease in phosphorylation of Rb at Ser780from 6 h onward, followed by reduced Rb levels at 24 h. |
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体内研究
(In Vivo) | Riviciclib hydrochloride (administered i.p.; 35 kg/mg daily for 10 days, in human xenograft mode with severe combined immunodeficient mice) shows significant inhibition in the growth of human colon carcinoma HCT-116 xenograft[3].
Riviciclib hydrochloride (administered via i.p.; 50 mg/kg once daily; 30 mg/kg twice daily for 18 treatments, in human xenograft mode with severe combined immunodeficient mice) significantly inhibited growth[3].
| Animal Model: | Human xenograft mode with HCT-116 tumor model (severe combined immunodeficient mice)[3] | | Dosage: | 35 mg/kg | | Administration: | Administered i.p.; daily for 10 days | | Result: | Given 35 mg/kg showed significant inhibition in the growth. |
| Animal Model: | Human xenograft model with H-460 tumor xenograft (severe combined immunodeficient mice)[3] | | Dosage: | 50 mg/kg; 30 mg/kg | | Administration: | Administered i.p.; 50 mg/kg once daily for 20 days; Administered i.p.; 30 mg/kg twice daily for 18 treatments | | Result: | Given 50 mg/kg and 30 mg/kg twice daily significantly inhibited growth. |
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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 : 50 mg/mL(114.08 mM;Need ultrasonic) H2O : 25 mg/mL(57.04 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.2815 mL | 11.4077 mL | 22.8154 mL | | 5 mM | 0.4563 mL | 2.2815 mL | 4.5631 mL | | 10 mM | 0.2282 mL | 1.1408 mL | 2.2815 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。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.75 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.75 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.75 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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