SU5416
SU5416 (CAS 204005-46-9), also known as Semaxanib, is a small molecule inhibitor designed to block vascular endothelial growth factor receptor (VEGFR2), particularly targeting Flk-1/KDR receptor tyrosine kinase signaling. SU5416 effectively inhibits VEGF-induced phosphorylation of Flk-1, thereby interfering with endothelial cell proliferation, angiogenesis, and subsequent tumor vascularization. Preclinical studies demonstrated suppression of tumor growth accompanied by angiogenesis inhibition. Additionally, SU5416 acts as an agonist of the aryl hydrocarbon receptor (AHR), modulating immune responses via induction of indoleamine 2,3-dioxygenase (IDO) and regulatory T cell differentiation. These properties suggest potential utility not only in cancer research but also in investigating autoimmune conditions and transplant tolerance.
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.
- 1. Sarah-Eve Lemay, Manon Mougin, et al. "Unraveling AURKB as a potential therapeutic target in pulmonary hypertension using integrated transcriptomic analysis and pre-clinical studies." Cell Rep Med. 2025 Feb 18;6(2):101964. PMID: 39933527
- 2. Meng Zhang, Haobo Li, et al. "Serum proteome profiling reveals HGFA as a candidate biomarker for pulmonary arterial hypertension." Respir Res 25, 418 (2024).
- 3. Sunder Neelakantan, Emilio A. Mendiola, et al. "Dissecting contributions of pulmonary arterial remodeling to right ventricular afterload in pulmonary hypertension." July 2024
- 4. Wusheng Xiao, Nishith Shrimali, et al. "Branched chain α-ketoacids aerobically activate HIF1α signaling in vascular cells."bioRxiv. 2024 May 30:2024.05.29.595538. PMID: 38853866
- 5. Peng Zhang, Denielli Da Silva Goncalves Bos, et al. "Reduced exercise capacity occurs before intrinsic skeletal muscle dysfunction in experimental rat models of pulmonary hypertension." Pulm Circ. 2024 Apr 4;14(2):e12358. PMID: 38576776
| Physical Appearance | A solid |
| Storage | Desiccate at -20°C |
| M.Wt | 238.28 |
| Cas No. | 204005-46-9 |
| Formula | C15H14N2O |
| Synonyms | Semaxinib; SU-5416; SU 5416 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥11.9 mg/mL in DMSO |
| Chemical Name | (3Z)-3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-1H-indol-2-one |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC(=C(N1)C=C2C3=CC=CC=C3NC2=O)C |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
HUVECs |
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Preparation method |
The 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. |
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Reacting condition |
0.01-100 μM; 2 days |
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Applications |
In 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]: | |
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Animal models |
Female BALB/c nu/nu mice bearing A375 cell xenografts |
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Dosage form |
1-25 mg/kg; i.p.; q.d., for 39 days |
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Applications |
In 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. |
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Other notes |
Please 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. |
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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. |
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| Description | Semaxanib (SU5416) is a potent and selective inhibitor of VEGFR(Flk-1/KDR) with an IC50 value of 1.23 μM. | |||||
| Targets | VEGFR | |||||
| IC50 | 1.23 μM | |||||
Quality Control & MSDS
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