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Riviciclib (Synonyms: P276-00 free base)
Riviciclib (P276-00 free base) 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 对 Cisplatin 耐药性细胞具有抗肿瘤活性。
Riviciclib Chemical Structure
CAS No. : 920113-02-6
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
Riviciclib 的其他形式现货产品:
Riviciclib hydrochloride
| 生物活性 |
Riviciclib (P276-00 free base) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively[1][2]. Riviciclib shows antitumor activity on cisplatin-resistant cells[3].
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| IC50 & Target[1] |
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CDK9- Cyclin T1
0.020 μM (IC50)
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cdk4-cyclin D1
0.063 μM (IC50)
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CDK1-Cyclin B
0.079 μM (IC50)
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cdk2-cyclin A
0.224 μM (IC50)
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cdk2-cyclin E
2.540 μM (IC50)
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cdk6-cyclin D3
0.396 μM (IC50)
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CDK9-cyclin H
2.900 μM (IC50)
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体外研究
(In Vitro) |
Riviciclib (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 (3-24 hours; 1.5 μM) reduces cyclin D1, Cdk4, and Rb levels in H-460 cells. Rb (retinoblastoma) phosphorylation at Ser780 decrease at 3 h[2].
Riviciclib shows activity in human cancer cell lines, such as colon carcinoma, osteosarcomal, cervical carcinoma, and bladder carcinoma cells[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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 Ser780 decrease 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 Ser780 from 6 h onward, followed by reduced Rb levels at 24 h. |
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体内研究
(In Vivo) |
Riviciclib (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 (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 inhibits growth[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
| 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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| Clinical Trial |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Roskoski R Jr,Cyclin-dependent protein kinase inhibitors including palbociclib as anticancer drugs.Pharmacol Res. 2016 May;107:249-275.
[2]. Joshi KS, et al. In vitro antitumor properties of a novel cyclin-dependent kinase inhibitor, P276-00. Mol Cancer Ther. 2007 Mar;6(3):918-25.
[3]. Joshi KS,et al. P276-00, a novel cyclin-dependent inhibitor induces G1-G2 arrest, shows antitumor activity on cisplatin-resistant cells and significant in vivo efficacy in tumor models. Mol Cancer Ther. 2007 Mar;6(3):926-34.
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