生物活性
Durvalumab (MEDI 4736) is an humanized anti-PD-L1 monoclonal antibody, it completely blocks the binding of PD-L1 to both PD-1 and CD80, with IC50s of 0.1 and 0.04 nM, respectively. Durvalumab inhibits tumor growth in mouse xenograft models of human melanoma (A375) and pancreatic (HPAC) tumour cell lines, via a T-cell-mediated mechanism. Durvalumab (5-0.01 mg/kg for NOD/SCID mice with HPAC tumor; 5-0.1 mg/kg for NOD/SCID mice with A375 tumor; administration i.p.; twice per week; for 3 weeks) significantly inhibits the tumor growth of both HPAC and A375 xenografts compared with an isotype-matched control antibody.
Durvalumab对鼠的PD-L1无活性。(适用于人源及非人源化小鼠)
化学数据
分子量 | |
分子式 | |
CAS号 | 1428935-60-7 |
纯度 | >99% |
溶解性(25°C) | PBS buffer |
储存和运输条件 | 4°C, protect from light 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。