SU9516是CDK2选择性抑制剂,IC50值为22nM,对CDK1/CDK4抑制力弱(IC50=40/200nM),对PKC、EGFR、p38MAPK等无抑制作用。
别名:666837-93-0
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.
体外实验* | |
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细胞系 | RKO cells and SW480 cells |
方法 | Seeding RKO cells and SW480 cells in replicates in 96-well plates at 1 × 104 cells/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 |
*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。
体内实验* | |
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动物模型 | |
配制 | |
剂量 | |
给药处理 |
*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。
分子量 | 241.25 |
分子式 | C13H11N3O2 |
CAS号 | 377090-84-1 |
溶解性(25°C) | DMSO 100 mM |
储存条件 |
粉末型式 -20°C 3年;4°C 2年 溶于溶剂 -80°C 6个月;-20°C 1个月 |
运输方式 | 冰袋运输,根据产品的不同,可能会有相应调整。 |
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
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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 |
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。
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