GSK2837808A

99.04%

GSK2837808A

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品牌：源叶(MedMol)

产品编号：S83361 一键复制产品信息

CAS号：1445879-21-9

分子式：C₃₁H₂₅F₂N₅O₇S

分子量：649.6213

别名：3-((3-(N-cyclopropylsulfamoyl)-7-(2,4-dimethoxypyrimidin-5-yl)quinolin-4-yl)amino)-5-(3,5-difluorophenoxy)benzoic acid

货号	规格	价格	上海	北京	珠海	重庆	武汉
S83361-5mg	99.04%	￥620.00 S83361-5mg ￥620.00 现货	3 1 3	-	-	-	1
S83361-10mg	99.04%	￥980.00 S83361-10mg ￥980.00 现货	1 1	-	-	-	-
S83361-25mg	≥98%	￥1610.00 S83361-25mg ￥1610.00 2-3天	0 货期：2-3天	-	-	-	-
S83361-100mg	≥98%	￥3740.00 S83361-100mg ￥3740.00 2-3天	0 货期：2-3天	-	-	-	-

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产品介绍参考文献质检证书(COA) 摩尔浓度计算器相关产品

产品描述：

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

靶点：

IC50: 2.6 nM (hLDHA), 43 nM (hLDHB);Dehydrogenase

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。

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。

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.539 ml	7.697 ml	15.394 ml
5 mM	0.308 ml	1.539 ml	3.079 ml
10 mM	0.154 ml	0.77 ml	1.539 ml
50 mM	0.031 ml	0.154 ml	0.308 ml