2. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. Reactive Oxygen Species (ROS)
  4. Anticancer agent 289

Anticancer agent 289 是一种 H2O2 响应性抗癌前药。 Anticancer agent 289 表现出 H2O2 诱导的 DNA 烷基化活性，能选择性抑制高 ROS 表达的癌细胞 (相较于非恶性细胞) 的增殖，并在体内显著抑制肿瘤生长且无可见毒性。Anticancer agent 289 可用于三阴性乳腺癌 (TNBC) 的研究。

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Anticancer agent 289

Anticancer agent 289 Chemical Structure

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Anticancer agent 289 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

Anticancer agent 289 (compound 10a) (0-200 μM, 48 小时)，对 MDA-MB-468 细胞表现出优先细胞毒性，其 IC50 为 5.1 μM；而对 MCF-10A 细胞的毒性较低，其 IC50 为 16.2 μM，高出约 3 倍[1]。
Anticancer agent 289 具有良好的水溶性 (74 μM)，在生理 pH 7.4 条件下具有中等渗透性 (logPe =−5.67)，且在酸性条件下 (pH 6.4 时 logPe 小幅增加至 -5.22) 被动扩散能力增强[1]。

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

Anticancer agent 289 相关抗体:

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.
体内研究
(In Vivo)

Anticancer agent 289 (compound 10a) (5.0 mg/kg，每日腹腔注射，连续 8 周) 在 MDA-MB-468 细胞诱导的异种移植瘤小鼠模型中，能选择性抑制肿瘤生长，同时不影响正常组织，表现出抗肿瘤活性且安全性良好[1]。
Anticancer agent 289 (15 mg/kg，单次腹腔注射) 在与其精确氘代类似物联合给药时，在 MDA-MB-468 细胞诱导的异种移植瘤小鼠模型中仍保持良好的安全性，能最大程度减少脱靶效应[1]。

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.
分子量

289.99

Formula

C12H18BCl2NO2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Anticancer agent 289 相关分类

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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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