2. Apoptosis
  3. c-Myc
  4. AGB-374

AGB-374 是一种具有口服活性的 NDUFS7 抑制剂。AGB-374 可使 NDUFS7 蛋白不稳定，通过靶向线粒体复合物 I 抑制氧化磷酸化。AGB-374 在体内可降低结肠癌细胞中 MYC 蛋白水平，延缓结肠癌同源小鼠模型中的肿瘤生长。AGB-374 可协同增强铜螯合剂对癌细胞的细胞毒性。AGB-374 可与铜螯合剂协同下调癌细胞中 MYC 和 NDUFS7 蛋白水平。AGB-374 可用于结肠癌的研究。

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AGB-374

AGB-374 Chemical Structure

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AGB-374 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

AGB-374 is an orally active NDUFS7 inhibitor. AGB-374 destabilizes NDUFS7 protein and inhibits oxidative phosphorylation by targeting mitochondrial complex I. AGB-374 reduces MYC protein levels in colon cancer cells in vivo and delays tumor growth in syngeneic mouse models of colon cancer. AGB-374 synergistically enhances the cytotoxicity of copper chelators against cancer cells. AGB-374 cooperates with copper chelators to downregulate MYC and NDUFS7 protein levels in cancer cells. AGB-374 can be used for the research of colon cancer[1].

体外研究
(In Vitro)

AGB-374 (0-10 μM; 6 days) 在 HCT116、MIA PaCa-2 和 PANC-1 细胞中与 JR4-187 (HY-182241) 或 JR5-26 (HY-173477) 表现出显著的细胞毒性协同作用[1]。
AGB-374 (10 μM; 24 h) 可下调 HCT116 细胞中 NDUFS7 蛋白的表达水平[1]。

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

AGB-374 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: HCT116, MIA PaCa-2, and PANC-1 cells
Concentration: 0, 0.12, 0.37, 1.1, 3.3, 10 μM
Incubation Time: 6 days
Result: Exhibited significant cytotoxic synergy with JR4 or JR5 in HCT116.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Decreased levels of NDUFS7 protein in HCT116 cells.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax AUC0-t AUC0-∞ T1/2 CL Bioavailability C0
Mice[1] 5 mg/kg i.v. / 2684 ng·h/mL 2688 ng·h/mL 3.5 h 31 mL/min/kg / 3850 ng/mL
Mice[1] 10 mg/kg p.o. 1640 ng/mL 2190 ng·h/mL 2194 ng·h/mL 2.7 h 76 mL/min/kg 40.8 % /
体内研究
(In Vivo)

AGB-374 (25 mg/kg；口服；48 小时内给药 3 次/每日一次；连续 15 天) 可显著降低 BALB/c 小鼠 CT26 结肠肿瘤中的 MYC 蛋白水平，抑制结肠肿瘤的生长，且不会引发全身毒性[1]。

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

Animal Model: BALB/c (female, 8-10 weeks old, subcutaneous implantation of CT26 murine colon carcinoma cells)[1]
Dosage: 25 mg/kg
Administration: p.o.; three doses over 48 hours/daily; 15 days
Result: Reduced mean relative MYC level/GAPDH to 0.38 in tumor tissue, compared to control mean of 0.96.
Reduced CTR1 protein levels in treated tumors compared to controls, but the reduction was not statistically significant.
Delayed tumor growth significantly.
Reduced mean final tumor weight significantly.
Observed no apparent signs of toxicity, behavioral changes, or body weight alterations throughout the study.
Revealed no microscopic or morphological abnormalities in liver, heart, kidney, and spleen via histopathological analysis.
Reduced MYC protein levels in tumor tissue compared to controls.
分子量

534.01

Formula

C19H27ClF3N3O5S2
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

AGB-374 相关分类

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  • 稀释计算器

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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:

AGB-374AGB374AGB 374c-MycMycNDUFS7 inhibitorHCT116 cellsBALB/c micecolon cancerInhibitorinhibitorinhibit

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目录号：
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