F-14512 (hydrochloride)

F-14512 hydrochloride is an anticancer agent that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 hydrochloride enhances the affinity of polyamines for DNA, thereby inhibiting topoisomerase II and achieving selective cellular uptake. F-14512 hydrochloride exhibits significant cytotoxicity against cells with high PTS activity and induces DNA damage. F-14512 hydrochloride demonstrates potent antitumor activity in the MX1 breast tumor xenograft model. F-14512 hydrochloride could be used to study breast cancer^[1]. In Vitro:F-14512 (0.001-100 μM) hydrochloride enters the cell through the polyamine transport system, in CHO cells with normal PTS, the IC₅₀ is 0.12 μM, while in CHO-MG cells with defective PTS, the IC₅₀ is 8.7 μM^[1].
F-14512 (72 h) hydrochloride demonstrates high potency in multiple human cell lines (median IC50 = 0.18 μM) and is particularly effective against cell lines such as MX-1, LOX-IMV1, and HL-60^[1].
F-14512 (1-100 μM, 1-24 h) hydrochloride induces DNA damage in A549 cells and exhibited stronger cytotoxicity in xrs6 cells with defective DNA repair^[1].
In Vivo:F-14512 (0.16-1.25 mg/kg, i.p., once daily for 2 weeks) hydrochloride exhibits outstanding anti-tumor activity in the MX-1 model^[1].