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Submit ReviewCGP 60474
Description: Potent cdk inhibitor
Chemical Name: 3-[[4-[2-[(3-Chlorophenyl)amino]-4-pyrimidinyl]-2-pyridinyl]amino]-1-propanol
Purity: ≥98% (HPLC)
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 II. 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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Product Datasheets
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
If you know of a relevant reference for CGP 60474, please let us know.
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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
Do you know of a great paper that uses CGP 60474 from Tocris? Please let us know.
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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.