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CGP 60474

Cat. No. 5471 1 Citation Submit a Review Datasheet / COA / SDS
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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)
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Biological Activity Technical Data Solubility Calculators Datasheets References

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.

Select a batch to recalculate based on the batch molecular weight:
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 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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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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