GSK2837808A

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

GSK2837808A  纯度: ≥99.0%

GSK2837808A 是有效和选择性的乳酸脱氢酶A (LDHA) 抑制剂,对 hLDHA 和 hLDHB的 IC50 值分别为 2.6 和 43 nM。

GSK2837808A

GSK2837808A Chemical Structure

CAS No. : 1445879-21-9

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥3001 In-stock
2 mg ¥1100 In-stock
5 mg ¥2100 In-stock
10 mg ¥3500 In-stock
25 mg ¥7200 In-stock
50 mg ¥11500 In-stock
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GSK2837808A 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Glycolysis Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Glucose Metabolism Compound Library

生物活性

GSK2837808A is a potent and selective lactate dehydrogenase A (LDHA) inhibitor with IC50s of 2.6 and 43 nM for hLDHA and hLDHB, respectively.

IC50 & Target

IC50: 2.6 nM (hLDHA), 43 nM (hLDHB)[1]

体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

649.62

Formula

C31H25F2N5O7S

CAS 号

1445879-21-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (76.97 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.85 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.85 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [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].

上海金畔生物科技有限公司 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [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.

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