Biological Activity
Potent, selective cdk2 inhibitor (IC50 values are 0.022, 0.04, 0.2, >10, >10, 18 and >100 μM for cdk2, cdk1, cdk4, PKC, p38, PDGFR and EGFR respectively). Inhibits pRb phosphorylation causing enhanced pRB/E2F complex formation and induces G1 and G2-M cell cycle arrest. Transcriptionally downregulates Mcl-1 and has antiproliferative, cytostatic and pro-apoptotic effects in vitro.
Compound Libraries
SU 9516 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 241.25 |
| Formula | C13H11N3O2 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 377090-84-1 |
| PubChem ID | 5289419 |
| InChI Key | QNUKRWAIZMBVCU-WCIBSUBMSA-N |
| Smiles | O=C2NC1=CC=C(OC)C=C1/C2=C/C3=CNC=N3 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 24.12 | 100 | |
| ethanol | 4.83 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 241.25. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 4.15 mL | 20.73 mL | 41.45 mL |
| 5 mM | 0.83 mL | 4.15 mL | 8.29 mL |
| 10 mM | 0.41 mL | 2.07 mL | 4.15 mL |
| 50 mM | 0.08 mL | 0.41 mL | 0.83 mL |
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References
References are publications that support the products' biological activity.
Lane et al (2001) A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells. Cancer Res. 61 6170 PMID: 11507069
Yu et al (2002) SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells. Biochem.Pharmacol. 64 1091 PMID: 12234612
Gao et al (2006) The three-substituted indolinone cyclin-dependent kinase 2 inhibitor 3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one (SU9516) kills human leukemia cells via down-regulation of Mcl-1 through a transcriptional m Mol.Pharmacol. 70 645 PMID: 16672643
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