CGP74514A

    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.


Chemical Structure

img
CGP74514A
CAS# 481724-82-7 (HCl)

Theoretical Analysis

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

Size Price Shipping out time Quantity
Inquire bulk and customized quantity

Pricing updated 2021-03-06. Prices are subject to change without notice.

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.

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

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).

HS Tariff Code:
2934.99.9001

Handling Instructions:

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

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.



Additional Information

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