CGP74514A

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

MedKoo CAT#: 406377

CAS#: 481724-82-7 (CGP74514A HCl salt)

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

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CGP74514A is 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

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Theoretical Analysis

MedKoo Cat#: 406377
Name: CGP74514A
CAS#: 481724-82-7 (CGP74514A HCl salt)
Chemical Formula: C19H25Cl2N7
Exact Mass:
Molecular Weight: 422.35
Elemental Analysis: C, 54.03; H, 5.97; Cl, 16.79; N, 23.21


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

Appearance:
white solid powder

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

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


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. The cytotoxic effect of emetine and CGP-74514A studied with the hollow fiber model and ArrayScan assay in neuroendocrine tumors in vitro. Anticancer Agents Med Chem. 2012 Sep;12(7):783-90. PubMed PMID: 22263790.