The proto-oncogene c-kit(CD117,stem cell factor receptor)is a transmembrane glycoprotein and a member of the type Ⅲ tyrosine kinase receptor family.This receptor is involved in the growth and the differentiation of haematopoietic stem cells,mast cells,melanocytes,germ cells and interstitial cells of Cajal.c-Kit is overexpressed in several human tumors,including small cell lung carcinomas,melanomas,seminomas and gastrointestinal stromal tumors(GISTs).To explore c-Kit-targeted drug,we have designed and synthesized five polyamides 1-5(Fig.1).Then,their recognition to c-Kit gene promoter sequence by using CD,SPR,MS,EMSA,techniques,and polyamides-mediated c–kit mRNA,protein and apoptosis of two types of cancer cells,human non-small cell lung cancer cell line A549 and human gastric cancer cell line SGC-7901,by using fluorescence confocal microscopy,RT-PCR,Western Blot techniques,the real-time cell electronic sensing(RT-CES),Wound Healing assays,have been examined,respectively.Results show that both 4 and 5 can strongly recognize DNA sequence of c-Kit gene promoter and induce apoptosis of two types of cancer cells,implying they have a potential as c-Kit-targeted cancer drugs.