1445879-21-9
| 中文名称 | 1445879-21-9 |
|---|---|
| 中文同义词 | 乳酸脱氢酶A(LDHA)抑制剂(GSK2837808A);化合物GSK2837808A;3-((3-(N-环丙基氨磺酰基)-7-(2,4-二甲氧基嘧啶-5-基)喹啉-4-基)氨基)-5-(3,5-二氟苯氧基)苯甲酸;GSK 2837808A,LDHA抑制剂 |
| 英文名称 | GSK2837808A |
| 英文同义词 | GSK2837808A;GSK 2837808A (GSK2837808A);3-[[3-[(Cyclopropylamino)sulfonyl]-7-(2,4-dimethoxy-5-pyrimidinyl)-4-quinolinyl]amino]-5-(3,5-difluorophenoxy)benzoic acid;Benzoic acid, 3-[[3-[(cyclopropylamino)sulfonyl]-7-(2,4-dimethoxy-5-pyrimidinyl)-4-quinolinyl]amino]-5-(3,5-difluorophenoxy)-;3-((3-(N-Cyclopropylsulfamoyl)-7-(2,4-dimethoxypyrimidin-5-yl)quinolin-4-yl)amino)-5-(3,5-difluorophenoxy)benzoic acid;Inhibitor,inhibit,LDH,Lactate Dehydrogenase,GSK2837808A,GSK-2837808A;3-[[3-(cyclopropylsulfamoyl)-7-(2,4-dimethoxypyrimidin-5-yl)-4-quinolyl]amino]-5-(3,5-difluorophenoxy)benzoic acid |
| CAS号 | 1445879-21-9 |
| 分子式 | C31H25F2N5O7S |
| 分子量 | 649.62 |
| EINECS号 | |
| 相关类别 | 细胞生物学试剂 |
| Mol文件 | 1445879-21-9.mol |
| 结构式 |  |
1445879-21-9 性质
| 沸点 | 783.5±70.0 °C(Predicted) |
|---|---|
| 密度 | 1.57±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | 3.81±0.10(Predicted) |
| 颜色 | 浅黄至黄色 |
| Target | Value |
|
hLDHA
(Cell-free assay) | 2.6 nM |
|
hLDHB
(Cell-free assay) | 43 nM |
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 (EC 50 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 (EC 50 =10 μM). It also reduces ECAR with EC 50 =10 μM. LDH inhibition by GSK2837808A alters multiple metabolic pathways in Snu398 cells.
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.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-100681 | 1445879-21-9 GSK2837808A | 1445879-21-9 | 2mg | 800元 |
| 2024/04/30 | HY-100681 | 1445879-21-9 GSK2837808A | 1445879-21-9 | 5mg | 1800元 |