2. Cell Cycle/DNA Damage
  3. CDK
  4. Riviciclib

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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Riviciclib hydrochloride) usually boasts enhanced water solubility and stability.

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Riviciclib Chemical Structure

Riviciclib Chemical Structure

CAS No. : 920113-02-6

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Other Forms of Riviciclib:

Riviciclib Related Antibodies

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

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Description

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)

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.

Riviciclib Related Antibodies

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.
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].

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.
Molecular Weight

401.84

Formula

C21H20ClNO5
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Riviciclib Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Riviciclib920113-02-6P276-00CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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