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)
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

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.

Select a batch to recalculate based on the batch molecular weight:
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 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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Keywords: SU 9516, supplier, Potent, cdk2, inhibitors, inhibits, Transcriptionally, downregulates, Mcl-1, proapoptotic, Cyclin-Dependent, Protein, Kinases, Bcl-2, Family, SU9516, Cyclin-dependent, Kinase, 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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In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.

Pathways for SU 9516

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