1445879-21-9
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- CAS号:
- 1445879-21-9
- 英文名:
- GSK2837808A
- 英文别名:
- GSK2837808A;GSK 2837808A
(GSK2837808A);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;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)-
- 中文名:
- 1445879-21-9
- 中文别名:
- 化合物GSK2837808A;GSK 2837808A,LDHA抑制剂;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
- CBNumber:
- CB73333612
- 分子式:
- C31H25F2N5O7S
- 分子量:
- 649.62
- MOL File:
- 1445879-21-9.mol
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1445879-21-9化学性质
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沸点:
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783.5±70.0 °C(Predicted)
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密度:
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1.57±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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形态:
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crystalline solid
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酸度系数(pKa):
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3.81±0.10(Predicted)
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1445879-21-9性质、用途与生产工艺
GSK 2837808A 是一种选择性的 LDHA (lactate dehydrogenase A) 的抑制剂，对hLDHA和hLDHB的IC50分别为2.6 nM和43 nM。
| Target | Value |
hLDHA
(Cell-free assay)
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2.6 nM
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hLDHB
(Cell-free assay)
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43 nM
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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.
1445879-21-9
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-100681 | 1445879-21-9
GSK2837808A | 1445879-21-9 | 2mg | 950元 |
| 2024/01/25 | HY-100681 | 1445879-21-9
GSK2837808A | 1445879-21-9 | 5mg | 1800元 |
1445879-21-9, 1445879-21-9 相关搜索:
- 药靶配体
- 抑制剂
- 细胞生物学试剂
- C31H25F2N5O7S
- GSK 2837808A,LDHA抑制剂
- 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
- 化合物GSK2837808A
- 乳酸脱氢酶A(LDHA)抑制剂(GSK2837808A)
- 1445879-21-9
- 3-[[3-(cyclopropylsulfamoyl)-7-(2,4-dimethoxypyrimidin-5-yl)-4-quinolyl]amino]-5-(3,5-difluorophenoxy)benzoic acid
- Inhibitor,inhibit,LDH,Lactate Dehydrogenase,GSK2837808A,GSK-2837808A
- 3-((3-(N-Cyclopropylsulfamoyl)-7-(2,4-dimethoxypyrimidin-5-yl)quinolin-4-yl)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-[(Cyclopropylamino)sulfonyl]-7-(2,4-dimethoxy-5-pyrimidinyl)-4-quinolinyl]amino]-5-(3,5-difluorophenoxy)benzoic acid
- GSK 2837808A
(GSK2837808A)
- GSK2837808A