Biological Activity
Potent dual cdk1/cdk2 inhibitor (IC50 values are 20 and 50 nM, respectively). Also displays low micromolar activity at PKCα. 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
1eq. HCl | 17.79 | 50 | |
DMSO | 35.58 | 100 |
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 solvent 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 products' biological activity.
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
Keywords: CGP 60474, supplier, CGP60474, dual, cdk1cdk2, inhibitors, inhibits, cyclin, dependent, protein, kinases, Cyclin-dependent, Kinase, Cyclin-dependent, Kinase, Tocris Bioscience