CGP60474 - CAS 164658-13-3
Catalog number: B0084-430557
Category: Inhibitor
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Molecular Formula:
C18H18ClN5O
Molecular Weight:
355.82
COA:
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Targets:
PKC | VEGFR
Description:
CGP60474 is a promising inhibitor of PKC with a high degree of selectivity versus other serine/threonine and tyrosine kinases and show competitive kinetics relative to ATP.
Purity:
>98%
Synonyms:
CGP-60474; CGP 60474
MSDS:
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InChIKey:
IYNDTACKOAXKBJ-UHFFFAOYSA-N
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)
Canonical SMILES:
C1=CC(=CC(=C1)Cl)NC2=NC=CC(=N2)C3=CC(=NC=C3)NCCCO
1.Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors.
Kuo GH;Deangelis A;Emanuel S;Wang A;Zhang Y;Connolly PJ;Chen X;Gruninger RH;Rugg C;Fuentes-Pesquera A;Middleton SA;Jolliffe L;Murray WV J Med Chem. 2005 Jul 14;48(14):4535-46.
On the basis of previous studies, we identified pyrazine-pyridine A as a potent vascular endothelial growth factor inhibitor and pyrimidine-pyridine B as a moderately potent cyclin dependent kinase (CDK) inhibitor. A proposed combination of CGP-60474 and compound B led to the discovery of [1,3,5]triazine-pyridine as a new series of potent CDK inhibitors. Palladium-catalyzed C-C bond formation reactions, particularly the Negishi coupling reaction, were used to assemble various triazine-heteroaryl analogues effectively. Among them, compound 20 displayed high inhibitory potency at CDK1 (IC(50) = 0.021 microM), CDK2, and CDK5 and submicromolar potency at CDK4, CDK6, and CDK7. Compound 20 also displayed high potency at GSK-3beta. It demonstrated potent antiproliferative activity on various tumor cell lines, including HeLa, HCT-116, U937, and A375. When 20 was administered intraperitoneally at 150 and 125 mg/kg to nude mice bearing human A375 xenografts, the compound produced a significant survival increase. Molecular docking studies were conducted in an attempt to enhance the understanding of the observed structure-activity relationship.
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CAS 164658-13-3 CGP60474

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