Name: Ki11502
Brand: TargetMol
SKU: T208725
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

10 mg

待询

10-14周

50 mg

待询

10-14周

生物活性

产品描述	Ki11502 is a multi-target receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGFβ/α receptors (with an IC50 of less than 10 nM). It specifically suppresses PDGFβ receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Additionally, Ki11502 induces apoptosis and exhibits significant antiproliferative effects against specific leukemia subgroups, including those with Imatinib-resistant mutations. It is particularly suitable for studying the role of PDGF in vascular diseases and the involvement of proteoglycans in atherosclerosis.
靶点活性	PDGFRβ:<10 nM, PDGFRα:<10 nM
体外活性	Ki11502 (0.1-1 nM; 2 天) 在携带激活的 FIP1 样 1/PDGFRα 融合基因的嗜酸性白血病 EOL-1 细胞中引起显著的生长抑制、G0/G1 细胞周期阻滞和凋亡 (Apoptosis)。Ki11502 (0.1-1 nM; 3 h) 有效降低 EOL-1 细胞中 p-PDGFRα 及其下游信号途径(包括 p-Akt、p-ERK 和 p-STAT5)的水平。
体内活性	Ki11502 (50 mg/kg; 灌胃; 每天 2 次，连用 5 天) 能完全抑制 SCID 小鼠中 EOL-1 肿瘤异种移植物细胞的增殖。