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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C12H18BCl2NO2
- Peso molecular:289.99
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
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.
-
Cell Line:MDA-MB-468 and MCF-10A cells
-
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
-
Incubation Time:48 h
-
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.
-
Animal Model:MDA-MB-468 cells (7.5×106) induced-female nude mice (8 weeks)[1]
-
Dosage:5.0 mg/kg
-
Administration:i.p. daily for 7 weeks
-
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).
-
Animal Model:MDA-MB-468 cells (2 × 106) induced-female nude mice (8 weeks)[1]
-
Dosage:15 mg/kg
-
Administration:i.p., once
-
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
-
Peso molecular 289.99
-
Fòrmula C12H18BCl2NO2
-
SMILES
CCC1=CC(N(CCCl)CCCl)=CC=C1B(O)O
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Anticancer agent 289 Related Classifications
HY-180260 Related Classifications
Powered by Bioz