GSK 2837808A

製品コードS8590 バッチS859001

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₃₁H₂₅F₂N₅O₇S

分子量

649.62

CAS No.

1445879-21-9

Solubility (25°C)*

体外

DMSO

100 mg/mL (153.93 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

5%DMSO 1 Corn oil

2.5mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	GSK 2837808A is a selective LDHA (lactate dehydrogenase A) inhibitor with IC50 of 2.6 nM and 43 nM for hLDHA and hLDHB, respectively.
in vitro	GSK 2837808A rapidly and profoundly inhibits lactate production rates in multiple cancer cell lines including hepatocellular and breast carcinomas. GSK 2837808A increases rates of oxygen consumption in hepatocellular carcinoma cells at dose up to 3 microM, while higher concentrations directly inhibits mitochondrial function. GSK 2837808A dose dependently potentiates PKM2 activity, inhibits proliferation of Snu398 cells and induces apoptosis in Snu398 cells.^[1]
in vivo	GSK 2837808A rapidly and profoundly inhibits lactate production rates in multiple cancer cell lines including hepatocellular and breast carcinomas. GSK 2837808A increases rates of oxygen consumption in hepatocellular carcinoma cells at dose up to 3 microM, while higher concentrations directly inhibits mitochondrial function. GSK 2837808A dose dependently potentiates PKM2 activity, inhibits proliferation of Snu398 cells and induces apoptosis in Snu398 cells.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MDA-MB-453 cells
	濃度	2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM
	反応時間	2 h, 6 h
	実験の流れ	MDA-MB-453 cells are cultured in normoxic (21% oxygen) or hypoxic (1%) conditions overnight in DMEM supplemented with 5% FBS. Medium is exchanged with physiological DMEM (5 mM glucose, 0.5 mM glutamine, no FBS) containing DMSO or GSK 2837808A at multiple concentrations and collected after 2 h for hypoxic cells and 6 h for normoxic cells. Lactate concentrations are quantified using a YSI 2900 Biochemistry Analyzer with a lactate oxidase probe.
動物実験	動物モデル	male CD mice, male Sprague–Dawley rats
	投薬量	50 mg/kg in rats, 100 mg/kg in mice, 0.25 mg/kg
	投与方法	Oral gavage, IV

参考

[1] Julia Billiard, et al. Cancer Metab. 2013 Sep 6;1(1):19.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Metabolic lactate production coordinates vasculature development and progenitor behavior in the developing mouse neocortex [ Nat Neurosci, 2022, 25(7):865-875]	PubMed: 35726058

Metabolic lactate production coordinates vasculature development and progenitor behavior in the developing mouse neocortex [ Nat Neurosci, 2022, 25(7):865-875]

PubMed: 35726058

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。