2. Cell Cycle/DNA Damage
  3. Topoisomerase DNA/RNA Synthesis
  4. F-14512

F-14512 is an anticancer agent that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 enhances the affinity of polyamines for DNA, thereby inhibiting topoisomerase II and achieving selective cellular uptake. F-14512 exhibits significant cytotoxicity against cells with high PTS activity and induces DNA damage. F-14512 demonstrates potent antitumor activity in the MX1 breast tumor xenograft model. F-14512 can be used to study breast cancer.

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F-14512

F-14512 Chemical Structure

CAS No. : 866874-63-7

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Based on 1 publication(s) in Google Scholar

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F-14512 Related Antibodies

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Description

F-14512 is an anticancer agent that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 enhances the affinity of polyamines for DNA, thereby inhibiting topoisomerase II and achieving selective cellular uptake. F-14512 exhibits significant cytotoxicity against cells with high PTS activity and induces DNA damage. F-14512 demonstrates potent antitumor activity in the MX1 breast tumor xenograft model. F-14512 can be used to study breast cancer[1].

In Vitro

F-14512 (0.001-100 μM) 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) 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) 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.

F-14512 Related Antibodies
In Vivo

F-14512 (0.16-1.25 mg/kg, i.p., once daily for 2 weeks) 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

641.75

Formula

C33H47N5O8
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (194.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5582 mL 7.7912 mL 15.5824 mL
5 mM 0.3116 mL 1.5582 mL 3.1165 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5582 mL 7.7912 mL 15.5824 mL 38.9560 mL
5 mM 0.3116 mL 1.5582 mL 3.1165 mL 7.7912 mL
10 mM 0.1558 mL 0.7791 mL 1.5582 mL 3.8956 mL
15 mM 0.1039 mL 0.5194 mL 1.0388 mL 2.5971 mL
20 mM 0.0779 mL 0.3896 mL 0.7791 mL 1.9478 mL
25 mM 0.0623 mL 0.3116 mL 0.6233 mL 1.5582 mL
30 mM 0.0519 mL 0.2597 mL 0.5194 mL 1.2985 mL
40 mM 0.0390 mL 0.1948 mL 0.3896 mL 0.9739 mL
50 mM 0.0312 mL 0.1558 mL 0.3116 mL 0.7791 mL
60 mM 0.0260 mL 0.1299 mL 0.2597 mL 0.6493 mL
80 mM 0.0195 mL 0.0974 mL 0.1948 mL 0.4869 mL
100 mM 0.0156 mL 0.0779 mL 0.1558 mL 0.3896 mL
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F-14512 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

F-14512866874-63-7F14512F 14512TopoisomeraseDNA/RNA SynthesisantitumorMX1 human breast tumor xenograft modelpolyamine transport systemPTSInhibitorinhibitorinhibit

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