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Submit ReviewSU 5416
说明： VEGFR inhibitor. Also inhibits KIT, RET, MET and FLT3
别名： Semaxinib
化学名： 3-[(3,5-Dimethyl-1H-pyrrol-2-yl)methylene]-1,3-dihydro-2H-indol-2-one
纯度： ≥99% (HPLC)
生物活性 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.
化合物库 for SU 5416
SU 5416 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
技术数据 for SU 5416
| 分子量 | 238.28 |
| 公式 | C15H14N2O |
| 储存 | Desiccate at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for SU 5416
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 23.83 | 100 |
制备储备液 for SU 5416
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for SU 5416
参考文献 for SU 5416
参考文献是支持产品生物活性的出版物。
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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关键词: 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 篇 SU 5416 的引用文献
引用文献是使用了 Tocris 产品的出版物。 SU 5416 的部分引用包括：
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
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
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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
