GSK2837808A|cas:1445879-21-9|西域试剂

GSK2837808A,99.0%

产品编号：Bellancom-100681| CAS NO：1445879-21-9| 分子式：C₃₁H₂₅F₂N₅O₇S| 分子量：649.62

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-100681	￥950.00	杭州北京（现货）
Bellancom-100681	￥1800.00	杭州北京（现货）
Bellancom-100681	￥2900.00	杭州北京（现货）
Bellancom-100681	￥5800.00	杭州北京（现货）
Bellancom-100681	￥9300.00	杭州北京（现货）

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GSK2837808A

产品介绍

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。

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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

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