CAS NO: | 1332331-08-4 |
GSK2194069 is a fatty acid synthase (FAS) inhibitor. GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of hFAS with an IC50of 7.7 ± 4.1 nM for the overall hFAS reaction. FAS is upregulated in some cancers, including prostate cancer. GSK2194069 was found to inhibit tumour growth in prostate cancer C42b cell xenografts generated in Nod-SCID-gamma mice. Cellular FAS inhibition reduced cell growth were also demonstrated in non-small-cell lung (A549) cancer cell lines with an average EC50of 15 ± 0.5 nM.
分子量 | 428.48 |
分子式 | C25H24N4O3 |
CAS号 | 1332331-08-4 |
纯度 | >98% |
溶解性(25°C) | DMSO: 5 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 | 2.3338 mL | 11.6692 mL | 23.3383 mL |
5 mM | 0.4668 mL | 2.3338 mL | 4.6677 mL |
10 mM | 0.2334 mL | 1.1669 mL | 2.3338 mL |