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SU-5416

SU-5416

  • CAT Number: I002575
  • CAS Number: 204005-46-9
  • Molecular Formula: C15H14N2O
  • Molecular Weight: 238.29
  • Purity: ≥95%
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Semaxanib (SU-5416)(CAT: I002575) is a potent and selective inhibitor of vascular endothelial growth factor receptor (VEGFR) subtype Flk-1/KDR, with an IC50 value of 1.23 μM. Notably, it demonstrates a 20-fold greater selectivity for VEGFR compared to platelet-derived growth factor receptor beta (PDGFRβ), and it exhibits negligible activity against epidermal growth factor receptor (EGFR), insulin receptor (InsR), and fibroblast growth factor receptor (FGFR). Through its targeted inhibition of VEGFR, Semaxanib holds potential for modulating angiogenesis and vascular processes, making it a promising candidate for anti-angiogenic therapies in conditions such as cancer and other VEGFR-related disorders.

Catalog Number I002575
CAS Number 204005-46-9
Molecular Formula

C15H14N2O

Purity 95%
Target c-RET
Solubility DMSO: ≤ 22.5 mg/mL
Storage Desiccate at -20°C
IC50 1.23 uM [1]
IUPAC Name (3Z)-3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-1H-indol-2-one
InChI InChI=1S/C15H14N2O/c1-9-7-10(2)16-14(9)8-12-11-5-3-4-6-13(11)17-15(12)18/h3-8,16H,1-2H3,(H,17,18)/b12-8-
InChIKey WUWDLXZGHZSWQZ-WQLSENKSSA-N
SMILES CC1=CC(=C(N1)C=C2C3=CC=CC=C3NC2=O)C
Reference

</br>1:The aryl hydrocarbon receptor is required for induction of p21cip1/waf1 expression and growth inhibition by SU5416 in hepatoma cells. O/’Donnell EF, Jang HS, Pearce M, Kerkvliet NI, Kolluri SK.Oncotarget. 2017 Apr 11;8(15):25211-25225. doi: 10.18632/oncotarget.16056. PMID: 28424418 Free PMC Article</br>2:Mechanisms of SU5416, an inhibitor of vascular endothelial growth factor receptor, as a radiosensitizer for colon cancer cells. Kim EH, Lee H, Jeong YK, Jung WG.Oncol Rep. 2016 Aug;36(2):763-70. doi: 10.3892/or.2016.4868. Epub 2016 Jun 10. PMID: 27373272 </br>3:Pneumonectomy combined with SU5416 induces severe pulmonary hypertension in rats. Happé CM, de Raaf MA, Rol N, Schalij I, Vonk-Noordegraaf A, Westerhof N, Voelkel NF, de Man FS, Bogaard HJ.Am J Physiol Lung Cell Mol Physiol. 2016 Jun 1;310(11):L1088-97. doi: 10.1152/ajplung.00023.2016. Epub 2016 Apr 1. PMID: 27036867 </br>4:Detrimental Impact of Vasopressin V2 Receptor Antagonism in a SU5416/Hypoxia/Normoxia-Exposed Rat Model of Pulmonary Arterial Hypertension. Goto I, Dohi K, Ogihara Y, Okamoto R, Yamada N, Mitani Y, Ito M.Circ J. 2016;80(4):989-97. doi: 10.1253/circj.CJ-15-1175. Epub 2016 Feb 29. PMID: 26924211 Free Article</br>5:Mechanisms for SU5416 as a radiosensitizer of endothelial cells. Kim EH, Kim MS, Jeong YK, Cho I, You SH, Cho SH, Lee H, Jung WG, Kim HD, Kim J.Int J Oncol. 2015 Oct;47(4):1440-50. doi: 10.3892/ijo.2015.3127. Epub 2015 Aug 21. PMID: 26314590 </br>6:Marked Strain-Specific Differences in the SU5416 Rat Model of Severe Pulmonary Arterial Hypertension. Jiang B, Deng Y, Suen C, Taha M, Chaudhary KR, Courtman DW, Stewart DJ.Am J Respir Cell Mol Biol. 2016 Apr;54(4):461-8. doi: 10.1165/rcmb.2014-0488OC. PMID: 26291195 </br>7:Determinants for in vivo antitumor effect of angiogenesis inhibitor SU5416 formulated in PEGylated emulsion. Ogawara K, Abe S, Un K, Yoshizawa Y, Kimura T, Higaki K.J Pharm Sci. 2014 Aug;103(8):2464-9. doi: 10.1002/jps.24071. Epub 2014 Jul 1. PMID: 24985750 </br>8:Effects of the vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitor SU5416 on in vitro cultures of Plasmodium falciparum. Hempel C, Hoyer N, Staalsø T, Kurtzhals JA.Malar J. 2014 May 28;13:201. doi: 10.1186/1475-2875-13-201. PMID: 24885283 Free PMC Article</br>9:A phase I dose escalation and pharmacodynamic study of SU5416 (semaxanib) combined with weekly cisplatin and irinotecan in patients with advanced solid tumors. Martin LK, Bekaii-Saab T, Serna D, Monk P, Clinton SK, Grever MR, Kraut EH.Onkologie. 2013;36(11):657-60. doi: 10.1159/000355665. Epub 2013 Oct 14. PMID: 24192770 </br>10:Treatment with anti-gremlin 1 antibody ameliorates chronic hypoxia/SU5416-induced pulmonary arterial hypertension in mice. Ciuclan L, Sheppard K, Dong L, Sutton D, Duggan N, Hussey M, Simmons J, Morrell NW, Jarai G, Edwards M, Dubois G, Thomas M, Van Heeke G, England K.Am J Pathol. 2013 Nov;183(5):1461-73. doi: 10.1016/j.ajpath.2013.07.017. PMID: 24160323

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