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Submit ReviewKi 8751 is a potent, selective inhibitor of VEGFR-2 tyrosine kinase (IC50 = 0.9 nM). Displays some inhibitory activity towards c-Kit, PDGFRα and FGFR-2 (IC50 values range from 40 to 170 nM) but is highly selective over other receptor tyrosine kinases (IC50 > 10000 nM for FGFR-2, EGFR and HGFR). Inhibits VEGF-stimulated proliferation of human umbilical vein endothelial cells (HUVEC) and inhibits tumor growth in vivo; antiangiogenic.
Ki 8751 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。
分子量 | 469.41 |
公式 | C24H18F3N3O4 |
储存 | Store at +4°C |
纯度 | ≥97% (HPLC) |
CAS Number | 228559-41-9 |
PubChem ID | 11317348 |
InChI Key | LFKQSJNCVRGFCC-UHFFFAOYSA-N |
Smiles | COC1=C(OC)C=C2C(OC3=CC=C(NC(=O)NC4=CC=C(F)C=C4F)C(F)=C3)=CC=NC2=C1 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 46.94 | 100 |
以下数据基于产品分子量 469.41。 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 | 2.13 mL | 10.65 mL | 21.3 mL |
5 mM | 0.43 mL | 2.13 mL | 4.26 mL |
10 mM | 0.21 mL | 1.07 mL | 2.13 mL |
50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
参考文献是支持产品生物活性的出版物。
Kubo et al (2005) Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumour activities of N-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas. J.Med.Chem. 48 1359 PMID: 15743179
If you know of a relevant reference for Ki 8751, please let us know.
关键词: Ki 8751, Ki 8751 supplier, Potent, selective, VEGFR-2, inhibitors, inhibits, Vascular, Endothelial, Growth, Factors, Receptors, KDR, Flt, Receptor, Tyrosine, Kinases, RTKs, Ki8751, VEGFR, 2542, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Ki 8751 的部分引用包括:
Marino et al (2018) Regulation of breast cancer induced bone disease by cancer-specific IKKβ. Oncotarget 9 16134 PMID: 29662632
Kawakami et al (2011) Investigation of a novel molecular descriptor for the lead optimization of 4-aminoquinazolines as vascular endothelial growth factor receptor-2 inhibitors: application for quantitative structure-activity relationship analysis in lead optimization. J Neurosci 21 1371 PMID: 21306896
Page et al (2019) Positive Feedback Defines the Timing, Magnitude, and Robustness of Angiogenesis. Cell Rep 27 3139 PMID: 31189101
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