HRA00129-C004 significantly inhibited the growth of c-Met expressing lung cancer, GC and CRC cell lines with the IC50 in sub nanomolar range. HRA00129-C004 was able to kill both EBC-1 (c-Met+) and SW480 (c-Met-) cells when co-cultured, which is speculated to be a critical factor of robust anti-tumor efficacy overcoming the heterogeneity of solid tumors. Treatment with 1, 3, 10 mg/kg HRA00129-C004 demonstrated dose-dependent anti-tumor efficacy in GC and CRC PDX models, with tumor growth inhibition rate (TGI%) between 66% and 107%. In NCI-H441 lung cancer CDX models, treatment with 1, 3, 10 mg/kg HRA00129-C004 could significantly inhibit the tumor growth (TGI%=106%, 107% and 109%), respectively.