.product-side h2 span {width: 50%;}.product-side h2 span.hover {}Related ProductsSKLB610SU 5402Pazopanib (GW-786034)ZM323881MotesanibNintedanib (BIBF 1120)Molarity CalculatorDilution Calculator SU5416VEGF receptor inhibitor and AHR agonistCatalog No.A3847SizePriceStockQty10mM (in 1mL DMSO)$60.00In stock 10mg$70.00In stock 50mg$190.00In stock 100mg$250.00In stock Tel: +1-832-696-8203Email: sales@apexbt.comWorldwide Distributors Add to CartBulk InquiryFree samples Check OutSample solution is provided at 25 µL, 10mM.Publications citing ApexBio ProductsNature.2017 Jan 19;541(7637):417-420.Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Related Compound Libraries DiscoveryProbe™ Bioactive Compound LibraryDiscoveryProbe™ Anti-cancer Compound LibraryDiscoveryProbe™ Kinase Inhibitor LibraryDiscoveryProbe™ Tyrosine Kinase Inhibitor LibraryQuality Control Quality Control & MSDS View current batch: 64321 Purity = 98.56% COA (Certificate Of Analysis) HPLC NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Purity = 98.00% COA (Certificate Of Analysis) HPLC NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Purity = 99.75% COA (Certificate Of Analysis) HPLC NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Purity = 99.32% COA (Certificate Of Analysis) HPLC NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Purity = 99.52% COA (Certificate Of Analysis) HPLC NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Chemical structure Biological ActivityDescriptionSemaxanib (SU5416) is a potent and selective inhibitor of VEGFR(Flk-1/KDR) with an IC50 value of 1.23 μM.TargetsVEGFRIC501.23 μMProtocolCell experiment [1]:Cell linesHUVECsPreparation methodThe solubility of this compound in DMSO is > 11.9 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.Reacting condition0.01 ~ 100 μM; 2 daysApplicationsIn HUVECs, SU5416 dose-dependently inhibited VEGF- and FGF-driven mitogenesis, with the IC50 values of 0.04 ± 0.02 μM and 50 μM, respectively. SU5416 showed > 1000-fold selectivity over VEGF- driven mitogenesis than FGF-driven mitogenesis.Animal experiment [1]:Animal modelsFemale BALB/c nu/nu mice bearing A375 cell xenograftsDosage form1 ~ 25 mg/kg; i.p.; q.d., for 39 daysApplicationsIn BALB/c nu/nu mice bearing A375 cell xenografts, SU5416 at the dose of 3 mg/kg/day significantly inhibited tumor growth. SU5416 at the dose of 25 mg/kg/day resulted in a > 85% inhibition of tumor growth with no mortality.Other notesPlease test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.References:[1]. Fong TA, Shawver LK, Sun L, Tang C, App H, Powell TJ, Kim YH, Schreck R, Wang X, Risau W, Ullrich A, Hirth KP, McMahon G. SU5416 is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) that inhibits tyrosine kinase catalysis, tumor vascularization, and growth of multiple tumor types. Cancer Res. 1999;59(1):99-106.SU5416 Dilution CalculatorConcentration (start)xVolume (start)=Concentration (final)xVolume (final) femtomolar picomolar nanomolar micromolar millimolar molar nanoliter microliter milliliter liter femtomolar picomolar nanomolar micromolar millimolar molar microliter milliliter liter C1V1C2V2calculateSU5416 Molarity CalculatorMass=ConcentrationxVolumexMW* picograms nanograms micrograms milligrams grams kilograms femtomolar picomolar nanomolar micromolar millimolar molar nanoliter microliter milliliter liter g/molcalculate Chemical Properties Cas No. 204005-46-9SDF Download SDF Synonyms Semaxinib;SU-5416;SU 5416 Chemical Name (3Z)-3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-1H-indol-2-one Canonical SMILES CC1=CC(=C(N1)C=C2C3=CC=CC=C3NC2=O)C Formula C15H14N2O M.Wt 238.28 Solubility ≥11.9 mg/mL in DMSO, Storage Desiccate at -20°CPhysical AppearanceA solidShipping ConditionEvaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon requestGeneral tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. BackgroundDescription: SU5416 was found to inhibit VEGF-dependent phosphorylation of the Flk-1 receptor in Flk-1-overexpressing NIH 3T3 cells with an IC50 of 1.04±0.53 mM Vascular endothelial growth factor (VEGF), which stimulates vasculogenesis and angiogenesis, is able to create new blood vessels during embryonic development, new blood vessels after injury, muscle following exercise, and new vessels (collateral circulation) to bypass blocked vessels. Semaxanib (SU5416), a tyrosine-kinase inhibitor drug designed by SUGEN as a cancer therapeutic, is a potent and selective synthetic inhibitor of the Flk-1/KDR VEGF receptor tyrosine kinase demonstrating antiangiogenic effects.Preclinical study: SU5416 was found to inhibit vascular endothelial growth factor-dependent mitogenesis of human endothelial cells. Moreover, systemic administration of SU5416 at nontoxic doses in mice resulted in the inhibition of subcutaneous tumor growth of cells derived from various tissue origins. The antitumor effect of SU5416 was accompanied by the appearance of pale white tumors, supporting its antiangiogenic property [1]. Another study showed that SU5416 was also an aryl hydrocarbon receptor (AHR) agonist with unique properties. Like TCDD, SU5416 favors induction of indoleamine 2,3 dioxygenase (IDO) in immunologically relevant populations such as dendritic cells in an AHR-dependent manner, leading to generation of regulatory T-cells in vitro. These characteristics lead us to suggest that SU5416 may be an ideal clinical agent for treatment of autoimmune diseases and prevention of transplant rejection, two areas where regulatory ligands of the AHR have shown promise [2].Clinical trial: As an anticancer agent, SU5416 went as far as Phase III clinical trials, but showed poor results. Its clical termination is based on the results from a planned interim efficacy and safety analyses of a large phase III study of standard chemotherapy with or without SU5416 in the treatment of patients with advanced stage colorectal cancer, which shows that the study will not achieve the defined trial  endpoints due to a lack of clinical benefit.References:[1] Fong TA, Shawver LK, Sun L, Tang C, App H, Powell TJ, Kim YH, Schreck R, Wang X, Risau W, Ullrich A, Hirth KP, McMahon G. SU5416 is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) that inhibits tyrosine kinase catalysis, tumor vascularization, and growth of multiple tumor types. Cancer Res. 1999;59(1):99-106.[2] Mezrich JD, Nguyen LP, Kennedy G, Nukaya M, Fechner JH, Zhang X, Xing Y, Bradfield CA. SU5416, a VEGF receptor inhibitor and ligand of the AHR, represents a new alternative for immunomodulation. PLoS One. 2012;7(9):e44547. doi: 10.1371/journal.pone.0044547.