SU9516 CAS: 666837-93-0
MF: C13H11N3O2
MW: 241.25
A selectively potent ATP-competitive inhibitor of CDKs.

SU9516 (CAS 666837-93-0)

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SU9516 is rated 5.0 out of 5 by 2.
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Nombres Alternativos: (Z)-3-((1H-imidazol-5-yl)methylene)-5-methoxyindolin-2-one
Solicitud: SU9516 is a selectively potent ATP-competitive inhibitor of CDKs
Número de CAS: 666837-93-0
Peso Molecular: 241.25
Fórmula Molecular: C13H11N3O2
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
* En el Certificado de Análisis específico de lote, puede encontrar información específica (como el contenido en agua).
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SU9516 is a 3-substituted indolinone compound displaying anti-proliferative and proapoptotic properties in tumor cells. SU9516 displays activity as a selectively potent ATP-competitive inhibitor of CDKs. It also shows no significant effect (IC50 >10 μM) on the activities of PKC, p38, PDGFRβ, or EGFR. SU9516 has an Inhibitory effect on proliferation of growth-factor stimulated colon carcinoma cells by binding to Cdk2 and preventing the phosphorylation of pRb and its dissociation from E2F. SU9516 is an inhibitor of Cdc2, Cdk2 and Cdk4.


References

1. Lane, M E., et al., 2001. A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells. Cancer research. 61(16): 6170-7. PMID: 11507069
2. Yu, Bo., et al., 2002. SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells. Biochemical pharmacology. 64(7): 1091-100. PMID: 12234612

Estado de Materia :
Solid
Solubilidad :
Soluble in DMSO (10 mg/ml), and ethanol (20 mM). Insoluble in water.
ALMACENAMIENTO :
Store at 4° C
Punto de Fusión :
220.28° C (Predicted)
Punto de ebullición :
601.52° C at 760 mmHg (Predicted)
Densidad :
1.38 g/cm3 (Predicted)
Indice de Refracción :
n20D 1.70 (Predicted)
IC50 :
Cdk2/A: IC50 = 22 nM; Cdk1/B: IC50 = 40 nM; Cdk4/D1: IC50 = 200 nM; PKC: IC50 = >10 µM ; p38: IC50 = >10 µM ; PDGFR: IC50 = 18 µM ; EGFR : IC50 = >100 µM ; ATP-dependent molecular chaperone HSP82: EC5050 = 1250 nM (Candida albicans ); Trypanosoma brucei: EC5050 = 180 nM
Valores de pK :
pKa: 12.20, pKb: 4.74
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
WGK Alemania :
3
PubChem CID :
Número MDL :
MFCD05865243
SMILES :
COC1=CC\\2=C(C=C1)NC(=O)/C2=C\\C3=CN=CN3

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SU9516 (CAS 666837-93-0)  Menciones del Producto

Ver como otros han utilizado SU9516 (CAS 666837-93-0). Haga click en la entrada de PubMed .

Citaciones 1 a 4 de un total de 4

PMID: # 25394488  Su, M. et al. 2015. Cell Death Differ. 22: 986-99.

PMID: # 24101496  Bogdanow, et al. 2013. Proc Natl Acad Sci U S A. 110: 17510-5.

PMID: # 20844576  Zydek, M. et al. 2010. PLoS Pathog. 6: -.

PMID: # 31740384  Pharmacol. Res. 104545.

Citaciones 1 a 4 de un total de 4
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