CGP74514A

WARNING: This product is for research use only, not for human or veterinary use.

Description:CGP74514A is a CDK1 inhibitor with potential anticancer activity. In U937 cells, CGP74514A - induced apoptosis (5 microM) became apparent within 4 hr and approached 100% by 24 hr. The pan- caspase inhibitor Boc-fmk and the caspase-8 inhibitor lETD-fmk opposed CGP74514A -induced caspase-9 activation and PARP degradation, but not cytochrome c or Smac/DIABLO release. CGP74514A -mediated apoptosis was substantially blocked by ectopic expression of full-length Bel- 2, a loop-deleted mutant Bcl-2, and Bcl-x(L). CGP74514A treatment (5 microM; 18 hr) resulted in increased p21(CIP1) expression, p27(KIP1) degradation, diminished E2F1 expression, and dephosphorylation of p34(CDC2). It also induced early (i.e., within 2 hr) inhibition of CDK1 activity and dephosphorylation of pRb, followed by pRb degradation, but did not block pRb phosphorylation at CDK2- and CDK4- specific sites. These findings indicate that the selective CDK1 inhibitor, CGP74514A , induces complex changes in cell cycle-related proteins in human leukemia cells accompanied by extensive mitochondrial damage, caspase activation, and apoptosis.

Price and Availability

CGP74514Ais not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 406377Name: CGP74514ACAS#: 481724-82-7 (HCl)Chemical Formula: C19H25Cl2N7Exact Mass: Molecular Weight: 422.35Elemental Analysis: C, 54.03; H, 5.97; Cl, 16.79; N, 23.21

Related CAS #:190653-73-7 (free base)481724-82-7 (HCl)

Synonym:CGP74514A; CGP-74514A; CGP 74514A.

IUPAC/Chemical Name:N2-((1R,2S)-2-aminocyclohexyl)-N6-(3-chlorophenyl)-9-ethyl-9H-purine-2,6-diamine hydrochloride

InChi Key:GDCXPZPXAWTYJM-LDXVYITESA-N

InChi Code:InChI=1S/C19H24ClN7.ClH/c1-2-27-11-22-16-17(23-13-7-5-6-12(20)10-13)25-19(26-18(16)27)24-15-9-4-3-8-14(15)21;/h5-7,10-11,14-15H,2-4,8-9,21H2,1H3,(H2,23,24,25,26);1H/t14-,15+;/m0./s1

SMILES Code:CCN1C=NC2=C(NC3=CC=CC(Cl)=C3)N=C(N[C@H]4[C@@H](N)CCCC4)N=C12.[H]Cl

Technical Data

Additional Information

  Related:481724-82-7 (CGP74514A HCl salt)190653-73-7 (CGP74514A free base).   

References

1: Larsson DE, Hassan SB, Oberg K, Granberg D. Thecytotoxic effect of emetine and CGP-74514A studied with the hollow fibermodel and ArrayScan assay in neuroendocrine tumors in vitro. AnticancerAgents Med Chem. 2012 Sep;12(7):783-90. PubMed PMID: 22263790.