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7ACC2

 
Catalog No.
B4868
MCT抑制剂
组合的产品项目
规格价格库存 数量
2mg
¥ 1,454.00
现货
5mg
¥ 2,272.00
现货
10mg
¥ 4,000.00
现货
50mg
¥ 13,636.00
现货

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A

背景

7ACC2, a carboxycoumarin derivative, is a potent inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 value of ~ 10 nM for lactate uptake in the human cervix carcinoma cell line SiHa. The family of MCT is composed of 14 members, among which only four isoforms (i.e. MCT1-4) have been documented to act as proton-linked transporters carrying short chain monocarboxylates such as lactate and pyruvate across cell membranes. In cancer cells, MCT1 and MCT4 are the most widely expressed, and MCT1 shows a better affinity for L-lactate than MCT4, enabling lactate entry into oxidative tumor cells. Thus, MCT1 blockade could serve as a potential therapeutic strategy to limit cancer progression. In addition, 7ACC2 is also a potent inhibitor of mitochondrial pyruvate transport, which interferes with pyruvate import into mitochondria and ultimately prevents extracellular lactate uptake as efficiently as a MCT1 inhibitor.

References:

1. Draoui N, Schicke O, Fernandes A, et al. Synthesis and pharmacological evaluation of carboxycoumarins as a new antitumor treatment targeting lactate transport in cancer cells. Bioorganic & Medicinal Chemistry, 2013, 21(22): 7107-7117.

2. Corbet C, Bastien E, Draoui N, et al. Interruption of lactate uptake by inhibiting mitochondrial pyruvate transport unravels direct antitumor and radiosensitizing effects. Nature Communications, 2018, 9(1): 1208.

化学属性

StorageStore at -20°C
M.Wt309.32
Cas No.1472624-85-3
FormulaC18H15NO4
Solubilityinsoluble in EtOH; insoluble in H2O; ≥47.5 mg/mL in DMSO
Chemical Name7-(benzyl(methyl)amino)-2-oxo-2H-chromene-3-carboxylic acid
SDFDownload SDF
Canonical SMILESOC(C(C(O1)=O)=CC2=C1C=C(N(C)CC3=CC=CC=C3)C=C2)=O
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试验操作

Cell experiment:[1]

Cell lines

SiHa cells

Reaction Conditions

72 h incubation

Applications

7ACC2 inhibited SiHa cells proliferation by reducing lactate uptake (an MCT1-dependent process), with an EC50 value of 0.22 μM.

Animal experiment:[1,2]

Animal models

A SiHa mouse xenograft model

Dosage form

3 mg/kg

Intraperitoneal administration

Applications

A single dose of 7ACC2 (3 mg/kg) to mice led to a Cmax of 1246 ng/ml (4 μM) in a very short time (Tmax = 10 min) associated with a plasma half-life of 4.5 h. 7ACC2 (3 mg/kg, q.d., for 5 and 10 days), when combined with radiotherapy, significantly delayed tumor growth in a SiHa mouse xenograft model.

Note

The technical data provided above is for reference only.

References:

1. Draoui N, Schicke O, Fernandes A, et al. Synthesis and pharmacological evaluation of carboxycoumarins as a new antitumor treatment targeting lactate transport in cancer cells. Bioorganic & Medicinal Chemistry, 2013, 21(22): 7107-7117.

2. Corbet C, Bastien E, Draoui N, et al. Interruption of lactate uptake by inhibiting mitochondrial pyruvate transport unravels direct antitumor and radiosensitizing effects. Nature Communications, 2018, 9(1): 1208.

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