7ACC2

立即咨询

7ACC2

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1472624-85-3

包装与价格：

包装	价格(元)
2mg	电议
5mg	电议
10mg	电议
50mg	电议

产品介绍

化学性质

Storage	Store at -20°C
M.Wt	309.32
Cas No.	1472624-85-3
Formula	C₁₈H₁₅NO₄
Solubility	insoluble in EtOH; insoluble in H2O; ≥47.5 mg/mL in DMSO
Chemical Name	7-(benzyl(methyl)amino)-2-oxo-2H-chromene-3-carboxylic acid
Canonical SMILES	OC(C(C(O1)=O)=CC2=C1C=C(N(C)CC3=CC=CC=C3)C=C2)=O
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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.

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 C_maxof 1246 ng/ml (4 μM) in a very short time (T_max= 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.