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Submit ReviewSU 5416
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)
Biological Activity for SU 5416
SU 5416, an angiogenesis inhibitor, is a potent vascular endothelial growth factor receptor tyrosine kinase 1/2 inhibitor (IC50 = 40 nM). SU 5416 also potently inhibits c-Kit, FLT3 and RET tyrosine kinases (IC50 values are 30 nM, 160 nM and 170 nM, respectively). SU 5416 shows inhibition of tumour growth and vascularization and can be used to generate an animal model of pulmonary arterial hypertension.
Compound Libraries for SU 5416
SU 5416 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for SU 5416
| 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 for SU 5416
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 23.83 | 100 |
Preparing Stock Solutions for SU 5416
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 for SU 5416
References for SU 5416
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
Ciuclan et al (2011) A novel murine model of severe pulmonary arterial hypertension. Am.J.Respir.Crit. Care Med. 184 1171 PMID: 21868504
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, semaxanib, semaxinib, Semaxinib, MET, Other, 3037, Tocris Bioscience
12 Citations for SU 5416
Citations are publications that use Tocris products. Selected citations for SU 5416 include:
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
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
Hurst (2017) TNFα drives pulmonary arterial hypertension by suppressing the BMP type-II receptor and altering NOTCH signalling. Nat Commun 8 14079 PMID: 28084316
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
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
Longchamp et al (2018) Amino Acid Restriction Triggers Angiogenesis via GCN2/ATF4 Regulation of VEGF and H2S Production. Cell 173 117 PMID: 29570992
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
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
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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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Angiogenesis in Cancer Poster
This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.
Pathways for SU 5416
