ICL-CCIC-0019 selectively inhibited CHKA activity with potent antiproliferative activities against a broad spectrum of human cancer cell lines (IC50: 0.27 ± 0.06 μM; mean GI50 of 8 cancer cell lines: 1.09 μM, range: 0.38–2.70 μM; GI50 range of 2 normal cell lines: 30–120 μM); ICL-CCIC-0019 caused rapid and sustained lipid synthesis inhibition by acting on CDP-choline pathway and also showed potent in vivo anti-tumor activity. Here, CHKA is linked to neoplasm.