CAS NO: | 1959605-73-2 |
MK204 is a potent and selective inhibitor of aldo-keto reductase family member 1B10 (AKR1B10). AKR1B10 is induced in several cancer types, in particular, hepatocellular carcinoma, and may be involved with drug resistance. MK204 appears to target a distinct AKR1B10 inner specificity pocket not present in the closely related aldose reductase. MK204 had an IC50value of 80 nM compared to an IC50value of 21.7 μM for aldose reductase.
分子量 | 714.22 |
分子式 | C16H9Br5ClNO4 |
CAS号 | 1959605-73-2 |
纯度 | >98% |
溶解性(25°C) | DMSO: 3 mg/mL clear (warmed) |
储存和运输条件 | 固体粉末: -20°C 冷藏长期储存 常温运输及临时存放 |
小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.4001 mL | 7.0006 mL | 14.0013 mL |
5 mM | 0.28 mL | 1.4001 mL | 2.8003 mL |
10 mM | 0.14 mL | 0.7001 mL | 1.4001 mL |