Ki16198  355025-13-7

Ki-16198
分子式：C24H25ClN2O5S   分子量：488.98
 
產(chǎn)品描述
Ki16198， Ki16425的甲酯, 是LPA 拮抗劑，抑制LPA1-和 LPA3誘導(dǎo)的肌醇磷酸產(chǎn)生，Ki分別為0.34 μM 和0.93 μM,對(duì)LPA2具有較弱的抑制作用,對(duì)LPA4, LPA5, LPA6沒有抑制活性。
靶點(diǎn)
LPA1
LPA3
       
IC50
0.34 μM (Ki)
0.93 μM (Ki)
       
體外研究
Ki16198 or Ki16425 substantially inhibits LPA1- and LPA3-mediated responses with a similar potency, with low potency to LPA2 and no activity to LPA4, LPA5 and LPA6. Ki16198 (10 μM) is also effective to inhibit migration and invasion responses to LPA in YAPC-PD cancer cell line with a potency similar to that of Ki16425. Ki16198 (10 μM) inhibits the LPA-induced expression of proMMP-9 protein and mRNA in YAPC-PD cells.Ki16198 (1 μM) inhibits the proliferation of lpa1Δ-1 and lpa1Δ+-1 cells by about 70%.
體內(nèi)研究
Ki16198 (2 mg/kg) significantly decreases the total metastatic node weight in the peritoneal cavity and ascites formation by 50% in YAPC-PD xenograft mouse model.Ki16198 (60 mg/kg orally) significantly inhibits lactate-induced limb lesions in rats.
溶解性
DMSO 96 mg/mL，水 <1 mg/mL，乙醇 35 mg/mL
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO