2. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. Reactive Oxygen Species (ROS)
  4. 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.

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

Anticancer agent 289

Anticancer agent 289 Chemical Structure

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Anticancer agent 289 Related Antibodies

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Description

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[1].

In Vitro

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.

Anticancer agent 289 Related Antibodies

Cell Viability Assay[1]

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.
In Vivo

Anticancer agent 289 (compound 10a) (5.0 mg/kg, i.p. daily for 8 weeks) selectively suppresses tumor growth while sparing normal tissues and has an antitumor activity with a favorable safety profile in a MDA-MB-468 cells-induced xenograft mice model[1].
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.
Molecular Weight

289.99

Formula

C12H18BCl2NO2
SMILES

CCC1=CC(N(CCCl)CCCl)=CC=C1B(O)O
Shipping

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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Anticancer agent 289 Related Classifications

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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:

Anticancer agent 289Anticancer agent289Anticancer agent-289Reactive Oxygen Species (ROS)H2O2-responsive anticancer prodrugH2O2-inducibleROStriple-negative breast cancerInhibitorinhibitorinhibit

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