GSK2837808A 纯度:>99.0% 2mg

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首页酶、辅酶及抑制剂MCE>

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GSK2837808A 纯度:>99.0% 2mg

市场价：: 1200.00

促销价：: ¥1200.00

货号：HY-100681

品牌：MCE

配送至：

北京朝阳

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商品介绍
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GSK2837808A 是有效和选择性的乳酸脱氢酶A (LDHA) 抑制剂，对LDHA 和 LDHB的 IC₅₀ 值分别为1.9 和14 nM。

Description

GSK2837808A is a potent and selective lactate dehydrogenase A (LDHA) inhibitor with IC₅₀s of 1.9 and 14 nM for LDHA and LDHB, respectively.

IC₅₀ & Target

IC50: 1.9 nM (LDHA), 1.9 nM (LDHB)^[1]

In Vitro

GSK2837808A rapidly and profoundly inhibits lactate production rates in multiple cancer cell lines including hepatocellular and breast carcinomas. The potency of GSK2837808A across 30 cancer cell lines with different LDHA and LDHB expression levels ranges from 400 nM to no effect (EC₅₀ reported as 30 μM). GSK2837808A potency does not correlate with LDHA, LDHB, or the total LDH expression levels. GSK2837808A inhibits lactate production in hypoxia but at higher concentrations than in normoxia (EC₅₀=10 μM). It also reduces ECAR with EC₅₀=10 μM. LDH inhibition by GSK2837808A alters multiple metabolic pathways in Snu398 cells^[1].

In Vivo

Clearance following IV infusion of GSK2837808A at 0.25 mg/kg is shown to be 69 mL/minute/kg in rats, which exceeds the animal liver blood flow. Oral dosing of GSK2837808A at 50 mg/kg in rats or 100 mg/kg in mice results in blood compound levels at or below the detection limit of 2.5 ng/mL^[1].

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (153.94 mM)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5394 mL	7.6968 mL	15.3936 mL
5 mM	0.3079 mL	1.5394 mL	3.0787 mL
10 mM	0.1539 mL	0.7697 mL	1.5394 mL

* Please refer to the solubility information to select the appropriate solvent.

References

[1]. Billiard J, et al. Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells. Cancer Metab. 2013 Sep 6;1(1):19.

Cell Assay ^[1]	Sixty thousand Snu398 cells per well are plated in 6-well tissue culture plates in RPMI-1640 medium supplemented with 2.5% charcoal-stripped FBS. Cells are allowed to attach overnight and then DMSO control or the indicated doses of LDHA inhibitor dissolved in DMSO are added directly to the wells. After 4 to 8 days of incubation in the indicated oxygen conditions, adherent cells are trypsinized, counted, and had their viability assessed by the trypan-blue exclusion method using the Vi-Cell XR Cell Viability Analyzer^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice: GSK2837808A is administered to male CD mice or male Sprague-Dawley rats orally or by intravenous (IV) infusion over 120 minutes into a femoral vein. Arterial blood samples are collected over time and GSK2837808A concentration is determined by liquid chromatography (LC)/MS/MS analysis^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Billiard J, et al. Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells. Cancer Metab. 2013 Sep 6;1(1):19.