SU 5416

Pricing Availability   Qty
Cat.No. 3037 - SU 5416 | C15H14N2O | CAS No. 204005-46-9
Description: VEGFR inhibitor. Also inhibits KIT, RET, MET and FLT3
Alternative Names: Semaxinib
Chemical Name: 3-[(3,5-Dimethyl-1H-pyrrol-2-yl)methylene]-1,3-dihydro-2H-indol-2-one
Purity: ≥99% (HPLC)
Datasheet
Citations (11)
Reviews (1)
Literature
Pathways

Biological Activity

Inhibitor of vascular endothelial growth factor receptor (VEGFR) that also inhibits other tyrosine kinases KIT, MET, FLT3 and RET. Displays no activity against EGFR, HER2, IGF1R and PDGFR. Inhibits tumor vascularization and growth of multiple tumor types.

Compound Libraries

SU 5416 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 238.28
Formula C15H14N2O
Storage Desiccate at -20°C
Purity ≥99% (HPLC)
CAS Number 204005-46-9
PubChem ID 5329098
InChI Key WUWDLXZGHZSWQZ-WQLSENKSSA-N
Smiles O=C2NC1=CC=CC=C1/C2=C/C3=C(C)C=C(C)N3

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 23.83 100

Preparing Stock Solutions

The following data is based on the product molecular weight 238.28. Batch specific molecular weights may vary from batch to batch due to the degree 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 4.2 mL 20.98 mL 41.97 mL
5 mM 0.84 mL 4.2 mL 8.39 mL
10 mM 0.42 mL 2.1 mL 4.2 mL
50 mM 0.08 mL 0.42 mL 0.84 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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

Fong et al (1999) SU5416 is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) that inhibits tyrosine kinase catalysis, tumor vascularisation, and growth of multiple tumor types. Cancer Res. 59 99 PMID: 9892193

Smolich et al (2001) The antiangiogenic protein kinase inhibitors SU5416 and SU6668 inhibit the SCF receptor (c-Kit) in a human myeloid leukemia cell line and in acute myeloid leukemia blasts. Blood 97 1413 PMID: 11222388

Mologni et al (2006) Inhibition of RET tyrosine kinase by SU5416. J.Mol.Endocrinol. 37 199 PMID: 17032739


If you know of a relevant reference for SU 5416, please let us know.

View Related Products by Product Action

View all VEGFR Inhibitors

Keywords: SU 5416, SU 5416 supplier, VEGFR, inhibits, inhibitors, c-kit, KIT, Ret, cMET, FLT3, Hepatocyte, Growth, Factor, Receptors, HGFR, RTK, Receptor, Tyrosine, Kinases, RTKs, Vascular, Endothelial, KDR, SU5416, Semaxinib, MET, Other, 3037, Tocris Bioscience

11 Citations for SU 5416

Citations are publications that use Tocris products. Selected citations for SU 5416 include:

Neto-Neves et al (2017) Chronic Embolic Pulmonary Hypertension Caused by Pulmonary Embolism and Vascular Endothelial Growth Factor Inhibition. Am J Pathol 187 700 PMID: 28183533

Long et al (2015) Selective enhancement of endothelial BMPR-II with BMP9 reverses pulmonary arterial hypertension. Nat Med 21 777 PMID: 26076038

Chabon et al (2014) Role of vascular endothelial growth factor signaling in Schistosoma-induced experimental pulmonary hypertension. J Neurophysiol 4 289 PMID: 25006448

Cavasin et al (2014) Reversal of severe angioproliferative pulmonary arterial hypertension and right ventricular hypertrophy by combined phosphodiesterase-5 and endothelin receptor inhibition. J Transl Med 12 314 PMID: 25425003

DiStefano et al (2014) KRIT1 protein depletion modifies endothelial cell behavior via increased vascular endothelial growth factor (VEGF) signaling. J Biol Chem 289 33054 PMID: 25320085

Happé et al (2016) Pneumonectomy combined with SU5416 induces severe pulmonary hypertension in rats. Am J Physiol Lung Cell Mol Physiol 310 L1088 PMID: 27036867

Hurst (2017) TNFα drives pulmonary arterial hypertension by suppressing the BMP type-II receptor and altering NOTCH signalling. Nat Commun 8 14079 PMID: 28084316

Meloche et al (2017) Implication of Inflammation and Epigenetic Readers in Coronary Artery Remodeling in Patients With Pulmonary Arterial Hypertension. Arterioscler Thromb Vasc Biol 37 1513 PMID: 28473439

Novitskiy et al (2010) Anti-vascular endothelial growth factor treatment in combination with chemotherapy delays hematopoietic recovery due to decreased proliferation of bone marrow hematopoietic progenitor cells. J Thorac Oncol 5 1410 PMID: 20683208

Azzi et al (2015) Desert Hedgehog/Patch2 Axis Contributes to Vascular Permeability and Angiogenesis in Glioblastoma. Pulm Circ 6 281 PMID: 26635611

Hempel et al (2014) Effects of the vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitor SU5416 on in vitro cultures of Plasmodium falciparum. Malar J 13 201 PMID: 24885283


Do you know of a great paper that uses SU 5416 from Tocris? Please let us know.

Reviews for SU 5416

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SU5416.
By Anonymous on 12/01/2017
Assay Type: In Vivo
Species: Mouse
Cell Line/Tissue: Also used in rat

We study rodent models of pulmonary hypertension where we inject SU5416 in addition to placing the animals in hypoxia to exacerbate the PH phenotype


Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


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
Angiogenesis in Cancer

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Pathways for SU 5416

VEGF

VEGF Signaling Pathway

VEGF signaling pathway is involved in embryonic vascular development (vasculogenesis) and in the formation of new blood vessel (angiogenesis). It also induces cell migration, proliferation and survival.