CAS NO: | 1883351-01-6 |
UPCDC30245 is an allosteric inhibitor of AAA ATPase p97, also called valosine containing protein (VCP). p97 is an integral component of the ubiquitin fusion degradation (UFD) pathway. It plays a role in degradation of misfolded proteins, Golgi membrane reassembly, membrane transport, myofibril assembly, autophagosome maturation, and cell division, and is overexpressed in many tumor types. UPCDC30245 has an IC50value of 27 nM, and has been shown to bind at the junction between the D1 and D2 domains of p97. UPCDC30245 has been used in cryo-ECM to show how such inhibitor binding prevents the confomational changes necessary for p97 function.
分子量 | 463.63 |
分子式 | C28H38FN5 |
CAS号 | 1883351-01-6 |
纯度 | >98% |
溶解性(25°C) | DMSO: 30 mg/mL clear |
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 | 2.1569 mL | 10.7845 mL | 21.5689 mL |
5 mM | 0.4314 mL | 2.1569 mL | 4.3138 mL |
10 mM | 0.2157 mL | 1.0784 mL | 2.1569 mL |