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Cat. No.: HY-182242

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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.

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Formule: C₁₉H₂₇ClF₃N₃O₅S₂
Masse moléculaire:534.01

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

AGB-374 Chemical Structure

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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.

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	C_max	AUC_0-t	AUC_0-∞	T_1/2	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.

Chemical Information

Masse moléculaire 534.01
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Rima Mouawad, et al. Copper Transporter 1‑Mediated Deregulation of Copper
Homeostasis Impacts MYC and Oxidative Phosphorylation Pathways and Increases the Sensitivity of Tumor Cells to Complex I Inhibitors.

Calculators

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Calculateur de dilution

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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