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

Riviciclib hydrochloride  (Synonyms: P276-00)

Cat. No.: HY-16559 Purity: 99.01%
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Riviciclib hydrochloride (P276-00) 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 hydrochloride (P276-00) shows antitumor activity on cisplatin-resistant cells.

For research use only. We do not sell to patients.

Riviciclib hydrochloride Chemical Structure

Riviciclib hydrochloride Chemical Structure

CAS No. : 920113-03-7

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10 mM * 1 mL in DMSO
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Based on 2 publication(s) in Google Scholar

Other Forms of Riviciclib hydrochloride:

Riviciclib hydrochloride 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 hydrochloride (P276-00) 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 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)

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 Ser780 decrease 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Riviciclib hydrochloride 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 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].

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

438.30

Formula

C21H21Cl2NO5
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

[H]Cl.O=C1C=C(C2=CC=CC=C2Cl)OC3=C([C@@H]4CCN(C)[C@H]4CO)C(O)=CC(O)=C31
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (114.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 25 mg/mL (57.04 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2815 mL 11.4077 mL 22.8154 mL
5 mM 0.4563 mL 2.2815 mL 4.5631 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.2815 mL 11.4077 mL 22.8154 mL 57.0386 mL
5 mM 0.4563 mL 2.2815 mL 4.5631 mL 11.4077 mL
10 mM 0.2282 mL 1.1408 mL 2.2815 mL 5.7039 mL
15 mM 0.1521 mL 0.7605 mL 1.5210 mL 3.8026 mL
20 mM 0.1141 mL 0.5704 mL 1.1408 mL 2.8519 mL
25 mM 0.0913 mL 0.4563 mL 0.9126 mL 2.2815 mL
30 mM 0.0761 mL 0.3803 mL 0.7605 mL 1.9013 mL
40 mM 0.0570 mL 0.2852 mL 0.5704 mL 1.4260 mL
50 mM 0.0456 mL 0.2282 mL 0.4563 mL 1.1408 mL
DMSO 60 mM 0.0380 mL 0.1901 mL 0.3803 mL 0.9506 mL
80 mM 0.0285 mL 0.1426 mL 0.2852 mL 0.7130 mL
100 mM 0.0228 mL 0.1141 mL 0.2282 mL 0.5704 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Riviciclib hydrochloride Related Classifications

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:

Riviciclib920113-03-7P276-00CDKApoptosisCyclin dependent kinaseInhibitorinhibitorinhibit

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