WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406377
CAS#: 481724-82-7 (HCl)
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.
MedKoo Cat#: 406377
CAS#: 481724-82-7 (HCl)
Chemical Formula: C19H25Cl2N7
Molecular Weight: 422.35
Elemental Analysis: C, 54.03; H, 5.97; Cl, 16.79; N, 23.21
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 firstname.lastname@example.org to inquire quote.
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
The following data is based on the product molecular weight 422.35 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
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.
481724-82-7 (CGP74514A HCl salt)
190653-73-7 (CGP74514A free base).