生物活性
Dinaciclib (SCH727965)是一种新型有效的CDK抑制剂，作用于CDK2， CDK5， CDK1和CDK9，IC50分别为1 nM， 1 nM， 3 nM和4 nM，也抑制胸甘(dThd) DNA摄入。Dinaciclib抑制CDK1和CDK9 效果差不多，但是抑制CDK2和CDK5效果则分别强12和14倍。Dinaciclib作用于A2780细胞，有效抑制的DNA复制，抑制胸甘(dThd)DNA摄入,IC50为4 nM。Dinaciclib 浓度大于6.25 nM时，强抑制Rb在Ser 807/811位点磷酸化。
化学数据
| 分子量 | 396.48 |
| 分子式 | C21H28N6O2 |
| CAS号 | 779353-01-4 |
| 纯度 | 99.20% |
| 溶解性（25°C） | DMSO 55 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 | A2780 cells |
| 方法 | dThd uptake growth inhibition assay.
A2780 cells were maintained in DMEM (Cellgro) plus 10% fetal bovine serum (HyClone) and passaged twice weekly by detaching the monolayer with trypsin-EDTA (Life Technologies). One hundred microliters of A2780 cells (5 × 103 cells) were added per well to a 96-well Cytostar-T plate (Amersham) and incubated for 16 to 24 hours at 37°C. Compounds were serially diluted in complete media plus 2% 14C-labeled dThd (Amersham). Media were removed from the Cytostar T plate; 200 μL of various compound dilutions were added in quadruplicate; and the cells were incubated for 24 hours at 37°C. Accumulated incorporation of radiolabel was assayed using scintillation proximity and measured on a TopCount (Packard/Perkin-Elmer Life Sciences). The percentage of dThd uptake inhibition, relative to a vehicle control, was calculated and plotted on log-linear plots to allow derivation of IC50 values. |
| 浓度 | 0~500nM |
| 处理时间 | 16 to 24 h |
| 动物实验 |
|---|
| 动物模型 | A2780 cells xenograft model in mice |
| 配制 | 20% hydroxypropyl-β-cyclodextran |
| 剂量 | 8, 16, 32, and 48 mg/kg daily for 10 d |
| 给药处理 | i.p. |
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 | 2.5222 mL | 12.611 mL | 25.222 mL |
| 5 mM | 0.5044 mL | 2.5222 mL | 5.0444 mL |
| 10 mM | 0.2522 mL | 1.2611 mL | 2.5222 mL |
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