SU 9516

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Cat.No. 2907 - SU 9516 | C13H11N3O2 | CAS No. 377090-84-1
Description: Potent cdk2 inhibitor
Chemical Name: (Z)-1,3-Dihydro-3-(1H-imidazol-4-ylmethylene)-5-methoxy-2H-indol-2-one
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Reviews
Literature

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

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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
ethanol 4.83 20
DMSO 24.12 100

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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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the biological activity of the product.

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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View all Cyclin-Dependent Protein Kinase Inhibitors

Keywords: SU 9516, SU 9516 supplier, Potent, cdk2, inhibitors, inhibits, Transcriptionally, downregulates, Mcl-1, proapoptotic, Cyclin-Dependent, Protein, Kinases, Bcl-2, Family, SU9516, Cyclin-dependent, Kinase, 2907, Tocris Bioscience

1 Citation for SU 9516

Citations are publications that use Tocris products. Selected citations for SU 9516 include:

Shi et al (2014) The FGF-1-specific single-chain antibody scFv1C9 effectively inhibits breast cancer tumour growth and metastasis. J Cell Mol Med 18 2061 PMID: 25124967


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Literature in this Area

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