CGP60474

CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively) . CGP60474 is a selective and ATP-competitive PKC inhibitor[1][2][3].

Product Specifications

CAS Number

[164658-13-3]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

CDK; PKC

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/CGP60474.html

Purity

98.90

Solubility

DMSO : ≥ 50 mg/mL

Smiles

ClC1=CC(NC2=NC=CC(C3=CC=NC(NCCCO)=C3)=N2)=CC=C1

Molecular Formula

C18H18ClN5O

Molecular Weight

355.82

Precautions

H302, H315, H319, H335

References & Citations

[1]Jorda R, et al. How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?. J Med Chem. 2018;61 (20) :9105-9120.|[2]Han HW, et al. LINCS L1000 dataset-based repositioning of CGP-60474 as a highly potent anti-endotoxemic agent. Sci Rep. 2018;8 (1) :14969. Published 2018 Oct 8.|[3]Stanetty P, 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.