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- 2025年12月05日
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- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
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货期：1-2天
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MedChemExpress LLC
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10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥2572.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥569.0 |
| 规格： | 5 mg | 产品价格： | ￥1800.0 |
| 规格： | 10 mg | 产品价格： | ￥2900.0 |
| 规格： | 25 mg | 产品价格： | ￥4800.0 |
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GSK2837808A
CAS No. : 1445879-21-9
MCE 国际站：GSK2837808A
产品活性：GSK2837808A 是有效和选择性的乳酸脱氢酶A (LDHA) 抑制剂，对 hLDHA 和 hLDHB的 IC50 值分别为 2.6 和 43 nM。
研究领域：Metabolic Enzyme/Protease
作用靶点：Lactate Dehydrogenase
In Vitro: 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.
In Vivo: 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.
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