CGP60474

CGP60474 is a 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.

Product information

CAS Number: 164658-13-3

Molecular Weight: 355.82

Formula: C18H18ClN5O

Synonym:

CGP-60474

CGP 60474

Chemical Name: 3-[[4-[2-[(3-Chlorophenyl)amino]-4-pyrimidinyl]-2-pyridinyl]amino]-1-propanol

Smiles: OCCCNC1=CC(=CC=N1)C1=CC=NC(NC2=CC(Cl)=CC=C2)=N1

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)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

CGP60474 (Compound A) is a potent VEGFR-2 inhibitor, with an IC50 of 84 nM. CGP60474 is also a PKC inhibitor, with competitive kinetics relative to ATP.

References:

1. Stanetty P, Hattinger G, Schnürch M, Mihovilovic MD. Novel and efficient access to phenylamino-pyrimidine type protein kinase C inhibitors utilizing a Negishi cross-coupling strategy. J Org Chem. 2005 Jun 24;70(13):5215-20. PubMed PMID: 15960526.
2. 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. Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors. J Med Chem. 2005 Jul 14;48(14):4535-46. PubMed PMID: 15999992.

Products are for research use only. Not for human use.