CAS NO: | 1445879-21-9 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
2mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | GSK2837808A is a potent and selectivelactate dehydrogenaseA (LDHA)inhibitor withIC50s of 2.6 and 43 nM for hLDHA and hLDHB, respectively. | ||||||||||||||||
IC50& Target | IC50: 2.6 nM (hLDHA), 43 nM (hLDHB)[1] | ||||||||||||||||
体外研究 (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 (EC50reported 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[1]. | ||||||||||||||||
体内研究 (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[1]. | ||||||||||||||||
分子量 | 649.62 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C31H25F2N5O7S | ||||||||||||||||
CAS 号 | 1445879-21-9 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(76.97 mM;Need ultrasonic) 配制储备液
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