1. Cell Cycle/DNA Damage
  2. Topoisomerase DNA/RNA Synthesis
  3. 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.

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F-14512 hydrochloride

F-14512 hydrochloride Chemical Structure

CAS No. : 866874-39-7

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Description

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MX-1 human breast cancer xenograft model established in homozygous female athymic nude mice[1]
Dosage: 0.16, 0.32, 0.63, 1.25 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 2 weeks
Result: Led to tumor regression dose-dependently.
Molecular Weight

787.60

Formula

C33H51Cl4N5O8

CAS No.
SMILES

O=C1[C@]2([H])[C@H](C3=CC(OC)=C(C(OC)=C3)O)C4=CC(OCO5)=C5C=C4[C@H]([C@@]2([H])CO1)NC(CNCCCNCCCCNCCCN)=O.Cl.Cl.Cl.Cl

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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F-14512 hydrochloride
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HY-106031A
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