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.
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- CAS No.: 468719-53-1
- 화학식: C24H31F3N4O9S2
- 분자량:640.65
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Biological Activity
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.
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Cell Line:LM05-E (epithelial), LM05-Mix (epithelial and fibroblastic)
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Concentration:1-50 μM
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Incubation Time:5 d
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Result:Reduced cellular viability in both LM05-E and LM05-Mix cells, with LM05-E cells showing greater responsiveness to treatment.
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.
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Animal Model:BALB/c (2-4 month old female; M05 spontaneous hormone-dependent mammary tumor model, inoculated with M05 tumor cells)[1]
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Dosage:1.2 mg/kg; 12 mg/kg
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Administration:i.p.; once daily; 5 days
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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.
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Animal Model:athymic BALB/c (female, 5-6 weeks of age)[2]
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Dosage:35 mg/kg; 50 mg/kg
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Administration:i.v.; on days 1, 3, and 5 of a 14-day cycle; 4 total cycles
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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.
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Animal Model:athymic BALB/c (female, 5-6 weeks of age)[2]
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Dosage:35 mg/kg; 70 mg/kg
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Administration:i.v.; on days 1, 3, and 5 of a 14-day cycle; 2 total cycles
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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).
Chemical Information
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CAS No. 468719-53-1
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분자량 640.65
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화학식 C24H31F3N4O9S2
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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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Synonyms
NSC710464
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Brantley E, et al. AhR ligand Aminoflavone inhibits α6-integrin expression and breast cancer sphere-initiating capacity. Cancer Lett. 2016;376(1):53-61. [Content Brief]
[2]. Stark K, et al. Reactivation of estrogen receptor α by vorinostat sensitizes mesenchymal-like triple-negative breast cancer to aminoflavone, a ligand of the aryl hydrocarbon receptor. PLoS One. 2013;8(9):e74525. Published 2013 Sep 13. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AFP464 Related Classifications
HY-16031A Related Classifications
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