Riviciclib
Based on 3 publication(s) in Google Scholar
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. Riviciclib shows antitumor activity on cisplatin-resistant cells.
For research use only. We do not sell to patients.
- CAS No.: 920113-02-6
- Formula: C21H20ClNO5
- Molecular Weight:401.84
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Riviciclib
More
Biological Activity
Description
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) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | IC50 |
0.58 μM
Compound: 28; P276-00
|
Antiproliferative activity against human HT-29 cells assessed as reduction in [3H]-thymidine incorporation after 48 hrs by liquid scintillation assay
Antiproliferative activity against human HT-29 cells assessed as reduction in [3H]-thymidine incorporation after 48 hrs by liquid scintillation assay
|
[PMID: 30733087] |
| Sf9 | IC50 |
2540 nM
Compound: 9; P276-00
|
Inhibition of human CDK2/cyclin E expressed in baculovirus infected Sf9 insect cells using retinoblastoma (792 to 928 residues) as substrate after 30 mins by gamma32P-ATP based scintillation counting analysis
Inhibition of human CDK2/cyclin E expressed in baculovirus infected Sf9 insect cells using retinoblastoma (792 to 928 residues) as substrate after 30 mins by gamma32P-ATP based scintillation counting analysis
|
[PMID: 27171036] |
| Sf9 | IC50 |
63 nM
Compound: 9; P276-00
|
Inhibition of human N-terminal GST-tagged CDK4/cyclin D1 expressed in baculovirus infected Sf9 insect cells using retinoblastoma (792 to 928 residues) as substrate after 30 mins by gamma32P-ATP based scintillation counting analysis
Inhibition of human N-terminal GST-tagged CDK4/cyclin D1 expressed in baculovirus infected Sf9 insect cells using retinoblastoma (792 to 928 residues) as substrate after 30 mins by gamma32P-ATP based scintillation counting analysis
|
[PMID: 27171036] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
-
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.
-
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.
In Vivo
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].
MedChemExpress (MCE) 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
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 920113-02-6
-
Molecular Weight 401.84
-
Formula C21H20ClNO5
-
SMILES
O=C1C=C(C2=C(Cl)C=CC=C2)OC3=C([C@H]4[C@H](CO)N(C)CC4)C(O)=CC(O)=C13
-
Synonyms
P276-00 free base
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
-
Journal Impact Factor
-
Most Recent
-
Pharmaceuticals (Basel)
Computational Modeling to Identify Drugs Targeting Metastatic Castration-Resistant Prostate Cancer Characterized by Heightened Glycolysis. [Abstract]2024 Apr 29;17(5):569. PMID: 38794139 -
Int J Mol Sci
Cyclin-Dependent Kinases (CDKs) and the Human Cytomegalovirus-Encoded CDK Ortholog pUL97 Represent Highly Attractive Targets for Synergistic Drug Combinations. [Abstract]2022 Feb 24;23(5):2493. PMID: 35269635 -
Elife
2020 Dec 7:9:e61405. PMID: 33284104
Protocols
-
Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Purity & Documentation
References
[1]. Roskoski R Jr,Cyclin-dependent protein kinase inhibitors including palbociclib as anticancer drugs.Pharmacol Res. 2016 May;107:249-275. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Riviciclib Related Classifications
HY-16559A Related Classifications
Powered by Bioz