1. Cell Cycle/DNA Damage Stem Cell/Wnt PI3K/Akt/mTOR Apoptosis
  2. CDK GSK-3 Apoptosis
  3. R547

R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively.

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

R547 Chemical Structure

R547 Chemical Structure

CAS No. : 741713-40-6

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 230 In-stock
Solution
10 mM * 1 mL in DMSO USD 230 In-stock
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5 mg USD 134 In-stock
10 mg USD 209 In-stock
50 mg USD 770 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively[1][2][3][4][5].

IC50 & Target[1]

Cdk1/cyclin B

2 nM (Ki)

CDK2/cyclinE

3 nM (Ki)

CDK4/cyclin D

1 nM (Ki)

cdk2/cyclin A

0.1 nM (IC50)

CDK2/cyclinE

0.4 nM (IC50)

Cdk1/cyclin B

0.2 nM (IC50)

CDK3/Cyclin E

0.8 nM (IC50)

CDK5/p35

0.1 nM (IC50)

cdk6/cyclin D3

4 nM (IC50)

CDK7/cyclin H

171 nM (IC50)

GSK-3α

46 nM (IC50)

GSK-3β

260 nM (IC50)

In Vitro

R547 effectively inhibits CDK1/cyclin B, CDK2/cyclin E, and CDK4/cyclin D1 (Ki = 1–3 nmol/L) and is inactive (Ki > 5,000 nmol/L) against a panel of >120 unrelated kinases in cell-free assays[4].
R547 effectively inhibits the proliferation of tumor cell lines independent of multidrug resistant status, histologic type, retinoblastoma protein, or p53 status, with IC50s <0.60 μM[4].
R547 reduces phosphorylation of the cellular retinoblastoma protein at specific CDK phosphorylation sites at the same concentrations that induced cell cycle arrest[4].
R547 has anti-proliferative activity in tumor cells independent of p53, retinoblastoma, or MDR status[4].
R547 blocks tumor cells in G1 plus G2 and induces apoptosis[4].
R547 induces apoptosis as measured by DNA fragmentation[4].
R547 inhibits phosphorylation of retinoblastoma protein in humantumor cells[4].

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

Cell Cytotoxicity Assay[4]

Cell Line: Human tumor cell lines (MDA-MB-468, MDA-MB-435, MCF-7, HCT116, SW480, RKO, HT-29, HCT15, H460a, C33A, DU145, OSA-CL, LOX, JEKO-1, REC-1)
Concentration: MTT assay
Incubation Time: 5 days
Result: Has potent in vitro antiproliferative activity.

Cell Cycle Analysis[4]

Cell Line: R547, HCT116
Concentration: 0.1 μM, 0.2 μM, 0.6 μM
Incubation Time: 20 hours
Result: Decrease in BrdUrd incorporation and in percentage S phase in a dose-dependent, indicative of a cell cycle block in G1-S plus G2-M.

Western Blot Analysis[4]

Cell Line: HCT116 cells
Concentration: 0.1 μM, 0.2 μM, 0.6 μM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Showed a band corresponding to a p48/retinoblastoma fragment that becomes more intense at 48 and 72 hours.
In Vivo

R547 has significant in vivo efficacy with daily oral and once weekly i.v. dosing[4].
R547 inhibits phosphorylation of retinoblastoma protein in tumors[4].

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

Animal Model: 13-14 weeks old female immunodeficient nude mice (23-25 g), with HCT116/H460a/MDA-MB-435/DU145/LOX/A549 cells xenograft[4]
Dosage: 40 mg/kg
Administration: Oral administration; daily; for 3-weeks
Result: Showed antitumor activity in all of the models in this study.
Molecular Weight

441.45

Formula

C18H21F2N5O4S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(N1CCC(NC2=NC(N)=C(C(C3=C(C(F)=CC=C3OC)F)=O)C=N2)CC1)(C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (226.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2653 mL 11.3263 mL 22.6526 mL
5 mM 0.4531 mL 2.2653 mL 4.5305 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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: ≥ 2.5 mg/mL (5.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.57%

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2653 mL 11.3263 mL 22.6526 mL 56.6316 mL
5 mM 0.4531 mL 2.2653 mL 4.5305 mL 11.3263 mL
10 mM 0.2265 mL 1.1326 mL 2.2653 mL 5.6632 mL
15 mM 0.1510 mL 0.7551 mL 1.5102 mL 3.7754 mL
20 mM 0.1133 mL 0.5663 mL 1.1326 mL 2.8316 mL
25 mM 0.0906 mL 0.4531 mL 0.9061 mL 2.2653 mL
30 mM 0.0755 mL 0.3775 mL 0.7551 mL 1.8877 mL
40 mM 0.0566 mL 0.2832 mL 0.5663 mL 1.4158 mL
50 mM 0.0453 mL 0.2265 mL 0.4531 mL 1.1326 mL
60 mM 0.0378 mL 0.1888 mL 0.3775 mL 0.9439 mL
80 mM 0.0283 mL 0.1416 mL 0.2832 mL 0.7079 mL
100 mM 0.0227 mL 0.1133 mL 0.2265 mL 0.5663 mL
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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.

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