2. Immunology/Inflammation Cytoskeleton Others Cell Cycle/DNA Damage
  3. Aryl Hydrocarbon Receptor Integrin Drug Intermediate DNA/RNA Synthesis
  4. AFP464

AFP464 (NSC710464) is a prodrug of Aminoflavone (HY-132974) and an agonist of the aryl hydrocarbon receptor (AhR). AFP464 downregulates the expression of α6-integrin (α6-integrin), inhibits breast tumor growth, reduces the population of tumor-initiating cells, disrupts mammosphere structure, induces the formation of mucin lake clusters, triggers DNA damage, and exerts antiproliferative activity. AFP464 is rapidly converted to Aminoflavone by nonspecific esterases in plasma and cell culture media. AFP464 is applicable to research related to breast cancer.

For research use only. We do not sell to patients.

AFP464

AFP464 Chemical Structure

CAS No. : 468719-53-1

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Description

AFP464 (NSC710464) is a prodrug of Aminoflavone (HY-132974) and an agonist of the aryl hydrocarbon receptor (AhR). AFP464 downregulates the expression of α6-integrin (α6-integrin), inhibits breast tumor growth, reduces the population of tumor-initiating cells, disrupts mammosphere structure, induces the formation of mucin lake clusters, triggers DNA damage, and exerts antiproliferative activity. AFP464 is rapidly converted to Aminoflavone by nonspecific esterases in plasma and cell culture media. AFP464 is applicable to research related to breast cancer[1][2].

In Vitro

AFP464 (1-50 μM; 5 d) exhibits dose-dependent cytotoxicity in LM05-E and LM05-Mix mouse breast cancer cells, with LM05-E cells being more sensitive[1].

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

AFP464 Related Antibodies

Cell Viability Assay[1]

Cell Line: LM05-E (epithelial), LM05-Mix (epithelial and fibroblastic)
Concentration: 1-50 μM
Incubation Time: 5 d
Result: Reduced cellular viability in both LM05-E and LM05-Mix cells, with LM05-E cells showing greater responsiveness to treatment.
In Vivo

AFP464 (12 mg/kg; i.p.; once daily; 5 days) significantly inhibits M05 breast tumor growth, reduces mammosphere formation capacity, and decreases the frequency of stem-like and α6-integrin positive tumor cells in BALB/c mice[1].
AFP464 (35-50 mg/kg; i.v.; on days 1, 3, and 5 of a 14-day cycle; 4 total cycles) produces 54-57% tumor growth inhibition in MDA-MB-468 breast cancer xenografts[2].
AFP464 (35-70 mg/kg; i.v.; on days 1, 3, and 5 of a 14-day cycle; 2 total cycles) does not inhibit tumor growth in MDA-MB-231 breast cancer xenografts, with 70 mg/kg being the MTD[2].

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

Animal Model: BALB/c (2-4 month old female; M05 spontaneous hormone-dependent mammary tumor model, inoculated with M05 tumor cells)[1]
Dosage: 1.2 mg/kg; 12 mg/kg
Administration: i.p.; once daily; 5 days
Result: Produced sustained, significant inhibition of M05 tumor growth, with median tumor surface remaining far lower than control levels through the study period.
Effectively decreased M05-tumor derived mammosphere formation.
Reduced the population of Lin(-)/CD29hi/CD24+ stem-like cells.
Significantly decreased the fraction of α6-integrin positive cells in tumors.
Showed no appreciable tumor growth inhibition at 1.2 mg/kg dose.
Animal Model: athymic BALB/c (female, 5-6 weeks of age)[2]
Dosage: 35 mg/kg; 50 mg/kg
Administration: i.v.; on days 1, 3, and 5 of a 14-day cycle; 4 total cycles
Result: Inhibited median tumor growth by 57% after 1 cycle.
Inhibited median tumor growth by 54% after 2 cycles.
Showed equivalent, statistically significant antitumor activity compared to vehicle control.
Was well tolerated by mice.
Animal Model: athymic BALB/c (female, 5-6 weeks of age)[2]
Dosage: 35 mg/kg; 70 mg/kg
Administration: i.v.; on days 1, 3, and 5 of a 14-day cycle; 2 total cycles
Result: Produced 0% tumor growth inhibition at both 35 mg/kg and 70 mg/kg doses.
Was well tolerated at 35 mg/kg dose.
Induced up to 15% body weight loss and 1 death out of 7 mice at 70 mg/kg dose, defining it as the maximum tolerated dose (MTD).
Molecular Weight

640.65

Formula

C24H31F3N4O9S2
CAS No.
SMILES

CS(=O)(O)=O.FC1=C2C(C(C=C(C3=CC(F)=C(C=C3)NC([C@@H](N)CCCCN)=O)O2)=O)=C(C(F)=C1C)N.CS(=O)(O)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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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:

AFP464468719-53-1NSC710464AFP 464AFP-464NSC 710464NSC-710464Aryl Hydrocarbon ReceptorIntegrinDrug IntermediateDNA/RNA SynthesisAhRDrug Iintermediatearyl hydrocarbon receptorMDA-MB-468breast cancerestrogen receptor αMDA-MB-231LM05-EARNTCYP1A1α6-integrinLM05-MixInhibitorinhibitorinhibit

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