生物活性
PR-104A is a corresponding alcohol that is systemically converted from PR-104 and a hypoxia-targeted anticancer agent with IC50 of 153 and 60 μM for wild-type CHO AA8 under aerobic and anoxic conditions. PR-104A itself showed modest but significant selectivity for anoxic cells. In a study, the estimated unbound human clearance of PR-104A was 211 L/h/70 kg, with a steady state unbound volume of 105 L/70 kg. The size equivalent unbound PR-104A clearance was 2.5 times faster in dogs, 0.78 times slower in rats and 0.63 times slower in mice, which may reflect reported species differences in PR-104A O-glucuronidation. PR-104A is glucuronidated by UGT2B7 with high specificity and appears to make a major contribution to clearance of PR-104A in humans.
化学数据
分子量 | 514.33 |
分子式 | C15H22BrN4O9S |
CAS号 | 680199-06-8 |
纯度 | >98% |
溶解性(25°C) | DMSO |
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 |
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
| 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。
储备液配制
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 | 1.9443 mL | 9.7214 mL | 19.4428 mL |
5 mM | 0.3889 mL | 1.9443 mL | 3.8886 mL |
10 mM | 0.1944 mL | 0.9721 mL | 1.9443 mL |