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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.
|Storage||Desiccate at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
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.
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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
12 Citations for SU 5416
Citations are publications that use Tocris products. Selected citations for SU 5416 include:
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
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
Longchamp et al (2018) Amino Acid Restriction Triggers Angiogenesis via GCN2/ATF4 Regulation of VEGF and H2S Production. Cell 173 117 PMID: 29570992
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
Hurst (2017) TNFα drives pulmonary arterial hypertension by suppressing the BMP type-II receptor and altering NOTCH signalling. Nat Commun 8 14079 PMID: 28084316
Long et al (2015) Selective enhancement of endothelial BMPR-II with BMP9 reverses pulmonary arterial hypertension. Nat Med 21 777 PMID: 26076038
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
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
Chabon et al (2014) Role of vascular endothelial growth factor signaling in Schistosoma-induced experimental pulmonary hypertension. J Neurophysiol 4 289 PMID: 25006448
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
Do you know of a great paper that uses SU 5416 from Tocris? Please let us know.
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