CGP 60474

Pricing Availability   Qty
Cat.No. 5471 - CGP 60474 | C18H18ClN5O | CAS No. 164658-13-3
Description: Potent cdk inhibitor
Chemical Name: 3-[[4-[2-[(3-Chlorophenyl)amino]-4-pyrimidinyl]-2-pyridinyl]amino]-1-propanol
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature

Biological Activity

Potent cyclin-dependent kinase (cdk) inhibitor (reported IC50 values are 3 - 80, 9.5, 13, 17 - 60, 200 and 220 nM for cdk2, cdk5, cdk9, cdk1, cdk4 and cdk7, respectively). Also inhibits PKCα in the low micromolar range. Displays reversible G1/S cell cycle arrest in U2-OS cells.

Compound Libraries

CGP 60474 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 355.82
Formula C18H18ClN5O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 164658-13-3
PubChem ID 644215
InChI Key IYNDTACKOAXKBJ-UHFFFAOYSA-N
Smiles OCCCNC1=NC=CC(C2=NC(NC3=CC(Cl)=CC=C3)=NC=C2)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 35.58 100
1eq. HCl 17.79 50

Preparing Stock Solutions

The following data is based on the product molecular weight 355.82. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.81 mL 14.05 mL 28.1 mL
5 mM 0.56 mL 2.81 mL 5.62 mL
10 mM 0.28 mL 1.41 mL 2.81 mL
50 mM 0.06 mL 0.28 mL 0.56 mL

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References

References are publications that support the biological activity of the product.

Stanetty et al (2005) Novel and efficient access to phenylamino-pyrimidine type protein kinase C inhibitors utilizing a Negishi cross-coupling strategy. J.Org.Chem. 70 5215 PMID: 15960526

Sielecki et al (2000) Cyclin-dependent kinase inhibitors: useful targets in cell cycle regulation. J.Med.Chem. 43 1 PMID: 10633033

Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987


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Keywords: CGP 60474, CGP 60474 supplier, CGP60474, dual, cdk1cdk2, inhibitors, inhibits, cyclin, dependent, protein, kinases, Cyclin-dependent, Kinase, 5471, Tocris Bioscience

1 Citation for CGP 60474

Citations are publications that use Tocris products. Selected citations for CGP 60474 include:

Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987


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Literature in this Area

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Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.