生物活性
AZD5438是一种有效的CDK1/2/9抑制剂，IC50为16 nM/6 nM/20 nM。对CDK5/6作用效果稍弱，也抑制GSK3β。
化学数据
| 分子量 | 371.46 |
| 分子式 | C18H21N5O2S |
| CAS号 | 602306-29-6 |
| 纯度 | >99% |
| 溶解性（25°C） | DMSO 64 mg/mL
Ethanol 54 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 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | MCF-7, MDA-MB-231, HCT-116, HT29, LoVo, SW620, Colo-205 cells line |
| 方法 | Measurement of Cell Proliferation
AZD5438 was tested against solid tumor cell lines as previously described. Briefly, cells were incubated for 48 h with AZD5438 at a range of concentrations. At the end of incubation, the cells were pulsed with 5-bromo-2′-deoxyuridine (BrdUrd) and the amount of DNA synthesis was measured. The IC50 for inhibition of proliferation was specifically determined independently of cell death. Multiple myeloma cell lines were seeded into 96-well plates in RPMI 1640 supplemented with 10% FCS and glutamine and dosed with AZD5438 for 72 h. Cell growth was measured using AlamarBlue (Invitrogen) and GI50 values were calculated with reference to pretreatment control values. |
| 浓度 | 0~10 μ M |
| 处理时间 | 72 h |
| 动物实验 |
|---|
| 动物模型 | human HX147 tumor xenografts in Swiss nude (nu/nu genotype; AstraZeneca) mice |
| 配制 | prepared in hydroxy-propyl-methyl-cellulose |
| 剂量 | 37.5-75 mg/kg once or twice daily for ~3 wk |
| 给药处理 | oral gavage |
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 | 2.6921 mL | 13.4604 mL | 26.9208 mL |
| 5 mM | 0.5384 mL | 2.6921 mL | 5.3842 mL |
| 10 mM | 0.2692 mL | 1.346 mL | 2.6921 mL |
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