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

R547 

Cat. No.: HY-10014 Purity: 99.66%
Handling Instructions

R547 is a potent, selective and oral orally bioavailable 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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 209 In-stock
Estimated Time of Arrival: December 31
10 mg USD 190 In-stock
Estimated Time of Arrival: December 31
50 mg USD 700 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

R547 is a potent, selective and oral orally bioavailable 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].

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].

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.

741713-40-6

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (113.26 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.2265 mL 1.1326 mL 2.2653 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.66%

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Keywords:

R547R 547R-547CDKGSK-3ApoptosisCyclin dependent kinaseGlycogen synthase kinase-3Glycogen synthase kinase 3cyclin-dependentkinasemultiplehumantumorInhibitorinhibitorinhibit

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R547
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HY-10014
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