Anticancer agent 289
Anticancer agent 289 is a H2O2-responsive anticancer prodrug. Anticancer agent 289 exhibits H2O2-inducible DNA-alkylating activity, selectively inhibits the proliferation of high ROS-expressing cancer cells over nonmalignant cells, markedly suppresses tumor growth without observable toxicity in vivo. Anticancer agent 289 can be used for triple-negative breast cancer (TNBC) research.
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- 화학식: C12H18BCl2NO2
- 분자량:289.99
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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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Help & FAQs
Biological Activity
Anticancer agent 289 (compound 10a) (0-200 μM, 48 h) exhibits preferential cytotoxicity toward MDA-MB-468 cells with an IC50 of 5.1 μM but MCF-10A cells with a 3-fold higher IC50 of 16.2 μM[1].
Anticancer agent 289 has a good aqueous solubility (74 μM) and moderate permeability (logPe =−5.67) at at physiological pH7.4, enhances a passive diffusion under acidic conditions (a modest increase (logPe =−5.22) at pH 6.4)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-468 and MCF-10A cells
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Concentration:0.049, 0.098, 0.195, 0.391, 0.781, 1.563, 3.125, 6.250, 12.5, 25, 50, 100 and 200 μM
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Incubation Time:48 h
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Result:Exhibited significant growth inhibition in MDA-MB-468cells,with an IC50 of 5.1 μM.
Observed a 3-fold higher IC50 of 15.2 μM.
Anticancer agent 289 (15 mg/kg, i.p., once) has favorable safety profile, minimizing off-target effects when combination with the precisely deuterated analogue in a MDA-MB-468 cells-induced xenograft mice model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MDA-MB-468 cells (7.5×106) induced-female nude mice (8 weeks)[1]
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Dosage:5.0 mg/kg
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Administration:i.p. daily for 7 weeks
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Result:Displayed significantly suppressed tumor growth approximately 11%.
Has a tumor growth inhibition rate (IR) value of 89%.
Inhibits tumor weights.
Caused no treatment-related mortality or adverse effects occurred, and steadily increased body weights.
Revealed no structural abnormalities or pathological changes (including liver, kidneys, spleen, lungs, heart).
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Animal Model:MDA-MB-468 cells (2 × 106) induced-female nude mice (8 weeks)[1]
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Dosage:15 mg/kg
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Administration:i.p., once
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Result:Revealed the presence of phase II metabolites, arising from glucuronidation of phenolic intermediates and exhibit a diagnostic M/M+5 isotopic pattern substrates for UDP-glucuronosyltransferase (UGT)-catalyzed conjugated with uridine diphosphate glucuronic acid.
Chemical Information
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분자량 289.99
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화학식 C12H18BCl2NO2
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SMILES
CCC1=CC(N(CCCl)CCCl)=CC=C1B(O)O
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Anticancer agent 289 Related Classifications
HY-180260 Related Classifications
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