1445879-21-9
1445879-21-9 结构式
基本信息
乳酸脱氢酶A(LDHA)抑制剂(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)-
物理化学性质
| 报价日期 | 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 |
| 2024/04/30 | HY-100681 | 1445879-21-9 GSK2837808A | 1445879-21-9 | 10mM * 1mLin DMSO | 2072元 |
常见问题列表
| 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.