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SU 9516

CDK/cyclin inhibitor
 
ALX-270-400-M005 5 mg 101.00 USD
 
ALX-270-400-M025 25 mg 354.00 USD
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Cell permeable, potent, selective and ATP-competitive inhibitor of CDK2/cyclin A (IC50=22nM), CDK1/cyclin B (IC50=40nM) and CDK4/cyclin D1 (IC50=200nM). Has no effect on the activity of PKC, p38, PDGFRβ and EGFR (IC50>10µM). Displays anti-proliferative and pro-apoptotic properties in tumor cells. Inhibits proliferation of growth factor-stimulated colon carcinoma cells by binding to CDK2 and thus preventing the phosphorylation of pRb and its dissociation from E2F.

Product Specification

Alternative Name:3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one
 
Formula:C13H11N3O2
 
MW:241.3
 
CAS:377090-84-1
 
Purity:≥95% (HPLC)
 
Appearance:Yellow to orange solid.
 
Solubility:Soluble in DMSO (10mg/ml).
 
Shipping:Shipped on Blue Ice
 
Long Term Storage:+4°C
 
Handling:Protect from light. Packaged under inert gas.
 
270-400
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270-400

Product Literature References

Novel pyrrolyllactone and pyrrolyllactam indolinones as potent cyclin-dependent kinase 2 inhibitors: X. Li, et al.; Bioorg. Med. Chem. Lett. 13, 1939 (2003), Abstract;
SU9516: biochemical analysis of cdk inhibition and crystal structure in complex with cdk2: D.J. Moshinsky, et al.; BBRC 310, 1026 (2003), Abstract;
SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells: B. Yu, et al.; Biochem. Pharmacol. 64, 1091 (2002), Abstract;
A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells: M.E. Lane, et al.; Cancer Res. 61, 6170 (2001), Abstract;

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