生物活性
SU9516是CDK2选择性抑制剂，IC50值为22nM，对CDK1/CDK4抑制力弱（IC50=40/200nM）。Treatment with SU9516 (5 μM) inhibited (P ≤ 0.05) both cdk2-specific (27–64%) and cdk4-specific (26–49%) phosphorylation of pRb in SW480 cells at all (24, 48, and 72 h) time points. RKO cells remained blocked in G2-M at 20 h post-serum induction and -addition of SU9516. SU9516 produced a dose-dependent G1 accumulation in EGF-stimulated cells.Treatment with 5 microM SU9516 prevented dissociation of pRb from E2F1 in all cell lines (HT-29>RKO>SW480). Treatment effects were time-dependent, demonstrating greater inhibition at 48 hr versus 24hr in HT-29 cells. Furthermore, E2F species were sequestered in complexes with p107, p130, DP-1, and cyclins A and E. After a 24-hr treatment with 5 microM SU9516, cyclin D1 and cdk2 levels decreased by 10-60%. Exposure of U937 and other leukemia cells to SU9516 concentrations > or =5 microM rapidly (i.e., within 4 h) induced cytochrome c release, Bax mitochondrial translocation, and apoptosis in association with pronounced down-regulation of the antiapoptotic protein Mcl-1.
化学数据
| 分子量 | 241.25 |
| 分子式 | C13H11N3O2 |
| CAS号 | 377090-84-1 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO 100 mM |
| 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 | RKO cells and SW480 cells |
| 方法 | Seeding RKO cells and SW480 cells in replicates in 96-well plates at 1 × 104cells/well and allowing to attach overnight. adding SU9516 in concentrations from 0.05 μM to 50.00 μM for 24 h, then washing the cells twice with PBS, and replenishing cells with complete media. Fixing the cells at 0, 4, and 7 days post-drug removal and assaying for protein levels using a modified SRB cytotoxicity assay.Fixing the cells in 10% trichloroacetic acid for 1 h, washing in distilled H2O, and staining in 0.4% SRB/acetic acid for 30 min. Then washing the cells in 0.1% acetic acid, solubilizing in 10 mM Tris (pH 9), and analyzing on a Bio-Rad 360 microplate reader at 595 nm. Repeating all experiments at least three times. |
| 浓度 | ~50 μM |
| 处理时间 | 24 hours |
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 | 4.1451 mL | 20.7254 mL | 41.4508 mL |
| 5 mM | 0.829 mL | 4.1451 mL | 8.2902 mL |
| 10 mM | 0.4145 mL | 2.0725 mL | 4.1451 mL |
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