KRC-00715 is an orally effective inhibitor of c-Met, exhibiting high selectivity with an IC50 of 9.0 nM. This compound specifically inhibits the growth of gastric cancer cell lines with high c-Met expression by inducing G1/S phase block, and reduces the activity of downstream signals, including Akt, Erk, and c-Met itself. In the gastric cancer cell line Hs746T, KRC-00715 demonstrates cytotoxicity with an IC50 of 39 nM and selectively inhibits the proliferation of cell lines that overexpress c-Met. Additionally, KRC-00715 decreases tumor size in Hs746T xenograft mouse models.

KRC-00715是一种高效的c-Met抑制剂，其IC 50值为39 nM，显示出显著的细胞毒性。在不同浓度(8、40、200、1000 nM；3小时；Hs746T、AGS)下，KRC-00715能够抑制c-Met的自磷酸化，并显著限制细胞增殖。特别是在c-Met高表达的细胞系中，如Hs746T细胞，KRC-00715表现出强效活性，并抑制了Akt与Erk的磷酸化。此外，KRC-00715在30 nM和300 nM浓度下对SNU-5的G1/S阻滞效应显著高于SNU-1，相关数值分别是72.53、64.54和73.62、83.64。

通过口服灌注方式 (p.o.)，每日一次，连续10天给予KRC-00715 (50mg/kg)，能有效抑制裸鼠体内Hs746T肿瘤体积的增长。