生物活性
AZD5153 is a potent bivalent triazolopyridazine based Bromodomain and Extraterminal (BET) Inhibitor, with IC50 value of 5 nM. AZD5153 could significantly disrupt BRD4 foci, with IC50 value of 1.7 nM in U2OS cells. AZD5153 could inhibit the proliferation of AML, MM, and DLBCL cell lines, with the majority of cell lines having a GI50 value < 25 nM. Furthermore, 200 nM AZD5153 could significantly decrease the level of mTOR pathway associated proteins in sensitive hematologic cancer cell lines (MOLP8, MV-4-11, OCILY19).
In AML, MM, and DLBCL xenografted tumor mouse models, oral administration of AZD5153 at the dose of 1, 2.5, and 5mg/kg could inhibit tumor growth in a dose dependent manner.
化学数据
| 分子量 | 479.6 |
| 分子式 | C25H33N7O3 |
| CAS号 | 1869912-39-9 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO ≥ 10 mg/mL |
| 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 | 2.0851 mL | 10.4254 mL | 20.8507 mL |
| 5 mM | 0.417 mL | 2.0851 mL | 4.1701 mL |
| 10 mM | 0.2085 mL | 1.0425 mL | 2.0851 mL |
