| 应用 |
A cell-permeable Flk-1 (VEGFR-2) and c-Kit inhibitor |
| 产品介绍 |
Ki8751是高活性VEGFR2选择性抑制剂，IC50为0.9 nM，比对c-Kit，PDGFRα和FGFR-2的抑制性高40倍，对EGFR，HGFR和 InsR几乎无活性。 |
| 备注 |
Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR. |
| 生化机理 |
Ki8751 is potent, selective inhibitor of VEGFR-2 tyrosine kinase (IC50 = 0.9 nM). Ki8751 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). Ki8751 inhibits VEGF-stimulated proliferation of human umbilical vein endothelial cells (HUVEC) and inhibits tumor growth in vivo; antiangiogenic. |
| 别名 |
Ki 8751;Ki-8751;N-(2,4-二氟苯基)-N'-[4-[(6,7-二甲氧基-4-喹啉基)氧基]-2-氟苯基]脲;Ki 8751;Ki-8751;N-(2,4-Difluorophenyl)-N'-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-fluorophenyl]urea |
