上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
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 |
|
是否有货 |
|
100 mg |
|
询价 |
|
250 mg |
|
询价 |
|
500 mg |
|
询价 |
|
* 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].
|
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
2.540 μM (IC50)
|
cdk6-cyclin D3
0.396 μM (IC50)
|
CDK9-cyclin H
2.900 μM (IC50)
|
|
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. |
|
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. |
|
Clinical Trial |
|
分子量 |
|
Formula |
|
CAS 号 |
|
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.
|
参考文献 |
-
[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.
|
所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务