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SU9516 (CAS 666837-93-0)

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Synonym:(Z)-3-((1H-imidazol-5-yl)methylene)-5-methoxyindolin-2-one
Application:A selectively potent ATP-competitive inhibitor of CDKs
CAS Number:666837-93-0
Molecular Weight:241.25
Molecular Formula:C13H11N3O2
Refer to Certificate of Analysis for lot specific data (including water content).
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Product NameCatalog #UnitPriceQtyAddFavorites
SU9516 sc-204905 5 mg $149
Description
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.
Technical Information
Physical State:Solid
Solubility:Soluble in DMSO (10 mg/ml), and ethanol (20 mM). Insoluble in water.
Storage:Store at 4° C
Melting Point:220.28 °C (Predicted)
Boiling Point:601.52 °C at 760 mmHg (Predicted)
Density:1.38 g/cm3 (Predicted)
Refractive Index: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
pK Values:pKa: 12.20, pKb: 4.74
Safety and Reference Information
WGK Germany:3
PubChem CID:5289419
MDL Number:MFCD05865243
SMILES:COC1=CC\2=C(C=C1)NC(=O)/C2=C\C3=CN=CN3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
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
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