SU 11274

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Cat.No. 4101 - SU 11274 | C28H30ClN5O4S | CAS No. 658084-23-2
Description: Selective inhibitor of MET kinase activity
Chemical Name: (3Z)-N-(3-Chlorophenyl)-3-[[3,5-dimethyl-4-[(4-methyl-1-piperazinyl)carbonyl]-1H-pyrrol-2-yl]methylene]-2,3-dihydro-N-methyl-2-oxo-1H-indole-5-sulfonamide
Purity: ≥97% (HPLC)
Datasheet
Citations (5)
Reviews
Literature

Biological Activity

Selective inhibitor of MET tyrosine kinase activity (IC50 = 0.01 μM in vitro). Reduces cell growth in a dose-dependent manner; induces cell cycle arrest and apoptosis. Abrogates cell motility and migration in vitro and tumor angiogenesis in vivo.

Compound Libraries

SU 11274 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 568.09
Formula C28H30ClN5O4S
Storage Store at -20°C
Purity ≥97% (HPLC)
CAS Number 658084-23-2
PubChem ID 9549297
InChI Key FPYJSJDOHRDAMT-KQWNVCNZSA-N
Smiles CC1=C(\C=C(C3=CC(S(N(C)C5=CC(Cl)=CC=C5)(=O)=O)=CC=C3N4)/C4=O)NC(C)=C1C(N2CCN(C)CC2)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 28.4 50

Preparing Stock Solutions

The following data is based on the product molecular weight 568.09. 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
0.5 mM 3.52 mL 17.6 mL 35.21 mL
2.5 mM 0.7 mL 3.52 mL 7.04 mL
5 mM 0.35 mL 1.76 mL 3.52 mL
25 mM 0.07 mL 0.35 mL 0.7 mL

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References

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

Sattler et al (2003) A novel small molecule Met inhibitor induces apoptosis in cells transformed by the oncogenic TPR-MET tyrosine kinase. Cancer Res. 63 5462 PMID: 14500382

Wang et al (2003) Potent and selective inhibitors of the Met [hepatocyte growth factor/scatter factor (HGF/SF) receptor] tyrosine kinase block HGF/SF-induced tumor cell growth. Mol.Cancer Ther. 2 1085 PMID: 14617781

Seiwert et al (2009) The MET receptor tyrosine kinase is a potential novel therapeutic target for head and neck squamous cell carcinoma. Cancer Res. 69 3021 PMID: 19318576


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View all MET Receptor Inhibitors

Keywords: SU 11274, SU 11274 supplier, SU11274, Supplier, c-Met, inhibitors, inhibits, MET, tyrosine, kinase, activity, met, receptors, Receptors, 4101, Tocris Bioscience

5 Citations for SU 11274

Citations are publications that use Tocris products. Selected citations for SU 11274 include:

Boyd et al (2013) Dissecting the role of human embryonic stem cell-derived mesenchymal cells in human umbilical vein endothelial cell network stabilization in three-dimensional environments. Tissue Eng Part A 19 211 PMID: 22971005

Shibasaki et al (2014) Differential regulation of c-Met signaling pathways for synovial cell function. J Transl Med 3 554 PMID: 25332857

Dai et al (2012) Disturbance of Ca2+ homeostasis converts pro-Met into non-canonical tyrosine kinase p190MetNC in response to endoplasmic reticulum stress in MHCC97 cells. J Biol Chem 287 14586 PMID: 22418436

Sullivan et al (2012) ATM and MET kinases are synthetic lethal with nongenotoxic activation of p53. Springerplus 8 646 PMID: 22660439

Jiang et al (2015) YangZheng XiaoJi exerts anti-tumour growth effects by antagonising the effects of HGF and its receptor, cMET, in human lung cancer cells. Blood 13 280 PMID: 26310485


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Literature in this Area

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Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases