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

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.

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

AGB-374

AGB-374 Chemical Structure

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AGB-374 Related Antibodies

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Description

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].

In Vitro

AGB-374 (0.12-10 μM; 6 days) exhibits significant cytotoxic synergy with JR4 or JR5 in HCT116, MIA PaCa-2, and PANC-1 cells[1].
AGB-374 (10 μM; 24 h) downregulates NDUFS7 protein levels in HCT116 cells[1].

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

AGB-374 Related Antibodies

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.
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 % /
In Vivo

AGB-374 (25 mg/kg; p.o.; 3 doses within 48 h/once daily; for 15 consecutive days) significantly reduces MYC protein levels in CT26 colon tumors of BALB/c mice, inhibits colon tumor growth, and causes no systemic toxicity[1].

MedChemExpress (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.
Molecular Weight

534.01

Formula

C19H27ClF3N3O5S2
SMILES

CC(S(=O)(C1=CC=C(C(F)=C1)S(=O)(N2CCN[C@H](C2)C(N3CCC(F)(CC3)F)=O)=O)=O)C.Cl
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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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AGB-374 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:

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

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