CGP60474CDKs and PKC inhibitor, potent CAS# 164658-13-3 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 164658-13-3 | SDF | Download SDF |
| PubChem ID | 644215 | Appearance | Powder |
| Formula | C18H18ClN5O | M.Wt | 355.82 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 50 mg/mL (140.52 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 3-[[4-[2-(3-chloroanilino)pyrimidin-4-yl]pyridin-2-yl]amino]propan-1-ol | ||
| SMILES | C1=CC(=CC(=C1)Cl)NC2=NC=CC(=N2)C3=CC(=NC=C3)NCCCO | ||
| Standard InChIKey | IYNDTACKOAXKBJ-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C18H18ClN5O/c19-14-3-1-4-15(12-14)23-18-22-9-6-16(24-18)13-5-8-21-17(11-13)20-7-2-10-25/h1,3-6,8-9,11-12,25H,2,7,10H2,(H,20,21)(H,22,23,24) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | 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. |
CGP60474 Dilution Calculator
CGP60474 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.8104 mL | 14.052 mL | 28.1041 mL | 56.2082 mL | 70.2602 mL |
| 5 mM | 0.5621 mL | 2.8104 mL | 5.6208 mL | 11.2416 mL | 14.052 mL |
| 10 mM | 0.281 mL | 1.4052 mL | 2.8104 mL | 5.6208 mL | 7.026 mL |
| 50 mM | 0.0562 mL | 0.281 mL | 0.5621 mL | 1.1242 mL | 1.4052 mL |
| 100 mM | 0.0281 mL | 0.1405 mL | 0.281 mL | 0.5621 mL | 0.7026 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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CGP60474 is a potent inhibitor of cyclin-dependent kinases (CDKs) with IC50 value of 17 nM for CDK1 [1]. It is also an inhibitor of Protein Kinase C (PKC) [1].
CDKs are a family of protein kinases regulating the cell cycle. PKC plays an important role in signal transductions, cellular proliferation and differentiation [2].
CGP60474 was highly selective for PKC than other serine/threonine and tyrosine kinases and showed competitive kinetics relative to ATP [2].
References:
[1]. Kuo GH, Deangelis A, Emanuel S, et al. Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors. J Med Chem, 2005, 48(14): 4535-4546.
[2]. Stanetty P, Hattinger G, Schnürch M, et al. Novel and efficient access to phenylamino-pyrimidine type protein kinase C inhibitors utilizing a Negishi cross-coupling strategy. J Org Chem, 2005, 70(13): 5215-5220
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Novel and efficient access to phenylamino-pyrimidine type protein kinase C inhibitors utilizing a Negishi cross-coupling strategy.[Pubmed:15960526]
J Org Chem. 2005 Jun 24;70(13):5215-20.
A novel, short, and efficient synthetic pathway to 3-{4-[2-(3-chlorophenylamino)-pyrimidin-4-yl]-pyridin-2-ylamino}-propanol (CGP 60474) and a series of analogues was developed. The synthetic sequence consisted of a Negishi-type cross-coupling reaction in the key step followed by two subsequent nucleophilic substitution reactions. This strategy represents a versatile and robust protocol to access diverse analogues of the title compound for subsequent SAR studies as potential phenylamino-pyrimidine type protein kinase C inhibitors.
