481724-82-7|CGP74514A|N2-((1R,2S)-2-aminocyclohexyl)-N6-(3-chlorophenyl)-9-ethyl-9H-purine-2,6-diamine hydrochloride|-范德生物科技公司

CGP74514A

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names：
N2-((1R,2S)-2-aminocyclohexyl)-N6-(3-chlorophenyl)-9-ethyl-9H-purine-2,6-diamine hydrochloride
CAS号：
481724-82-7
MDL Number：
MF(分子式)： C19H25Cl2N7 MW(分子量)： 422.35
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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询价

中文别名	CGP74514A
英文别名	CGP74514A; CGP-74514A; CGP 74514A.
CAS号	481724-82-7
Inchi	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
InchiKey	GDCXPZPXAWTYJM-LDXVYITESA-N
分子式 Formula	C19H25Cl2N7
分子量 Molecular Weight	422.35
溶解度Solubility
性状	white solid powder
储藏条件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

产品说明	CGP74514A(CAS:481724-82-7 ):仅限应用于工业或者科学研究过程中非医疗目的，不应用于人类或动物的临床诊断以及治过程疗，该产品非药用，非食用。
Introduction	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.
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警示图
危险性	Warning
危险性警示
安全声明
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备注

[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.