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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

分子式: C₁₉H₂₇ClF₃N₃O₅S₂
分子量:534.01

保管条件:

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

AGB-374 構造式

容量

価格（税別）

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生物活性
- 製品説明
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

体外実験

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 %	/

体内実験

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.

化学情報

分子量 534.01
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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.

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100 mg

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