中文名 | GSK2837808A |
英文名 | GSK2837808A |
别名 | 化合物GSK2837808A 乳酸脱氢酶A(LDHA)抑制剂(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 |
英文别名 | GSK2837808A GSK 2837808A(GSK2837808A) 3-((3-(N-Cyclopropylsulfamoyl)-7-(2,4-dimethoxypyrimidin-5-yl)quinolin-4-yl)amino)-5-(3,5-difluorophenoxy)benzoic acid 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)- |
CAS | 1445879-21-9 |
化学式 | C31H25F2N5O7S |
分子量 | 649.62 |
密度 | 1.57±0.1 g/cm3(Predicted) |
沸点 | 783.5±70.0 °C(Predicted) |
溶解度 | DMSO: ≥ 100 mg/mL |
酸度系数 | 3.81±0.10(Predicted) |
存储条件 | -20℃ |
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 (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. |
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. |
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 |
5 mM | 0.031 ml | 0.154 ml | 0.308 ml |
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