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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 for CGP 60474
CGP 60474 is a 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.
Technical Data for CGP 60474
| 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 for CGP 60474
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 35.58 | 100 | |
| 1eq. HCl | 17.79 | 50 |
Preparing Stock Solutions for CGP 60474
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 for CGP 60474
References for CGP 60474
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, Non-selective, CDKs, 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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