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别名 MK-8776, MK 8776
SCH900776 (MK-8776) 是一种靶向细胞周期检查点激酶 1(Chk1) 的抑制剂,IC50值为 3 nM。它比对 CDK2 和 Chk2 的选择性分别高 50 和 500 倍,具有潜在的放射增敏和化学增敏活性。

SCH900776 (MK-8776) 是一种靶向细胞周期检查点激酶 1(Chk1) 的抑制剂,IC50值为 3 nM。它比对 CDK2 和 Chk2 的选择性分别高 50 和 500 倍,具有潜在的放射增敏和化学增敏活性。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 329 | In stock | |
| 5 mg | ¥ 787 | In stock | |
| 10 mg | ¥ 1,430 | In stock | |
| 25 mg | ¥ 3,150 | In stock | |
| 50 mg | ¥ 4,520 | In stock | |
| 100 mg | ¥ 6,350 | In stock | |
| 200 mg | ¥ 8,560 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 865 | In stock |
SCH900776 相关产品
| 产品描述 | SCH900776 (MK-8776) is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities. |
| 靶点活性 | Chk1:3 nM, Chk2:1500 nM, CDK2:0.16 μM |
| 体外活性 | 在吉西他滨后30分钟给药,4 mg/kg SCH 900776足以诱导γ-H2AX生物标志物,而8 mg/kg SCH 900776增强肿瘤药效动力学和退化响应.递增剂量16 mg/kg和32 mg/kg的SCH 900776诱导肿瘤响应持续改进.重要的是,在BALB/c小鼠体内,SCH 900776剂量与强的生物标志物活化相关,而提高的肿瘤响应与吉西他滨对血液学指标增强的毒性无关. |
| 体内活性 | 羟基脲暴露24小时后,SCH 900776诱导DNA复制能力的剂量依赖性丧失。SCH 900776增强γ-H2AX对羟基脲,5-氟尿嘧啶和阿糖孢苷的响应。SCH 900776与抗代谢物结合,在2小时内诱导γ-H2AX的累积,表明复制叉瓦解和并且双链DNA断裂。此外,SCH 900776以剂量依赖的方式抑制Chk1 pS296自磷酸化的积累。SCH 900776是Chk2和CDK2的低效抑制剂,IC50分别为1.5 μM和0.16 μM。SCH 900776对细胞色素P450人肝微粒体亚型1A2,2C9,2C19,2D6和3A4没有明显的抑制作用。 |
| 激酶实验 | The Millipore Kinase Profiler service is used to generate general selectivity data for SCH 900776 against a broad range of serine/threonine and tyrosine kinases. Assays are typically run at two concentrations of SCH 900776 (0.5 and 5 μM), at a fixed (10 μM) concentration of ATP. Data are provided as percent activity remaining, relative to uninhibited controls. |
| 细胞实验 | For cell growth assays, cells are seeded at low density (500-1000 cells) in 96-well plates and then incubated with drug for 24 h (8 wells per concentration). Following treatment, cells are washed and grown in fresh media for 5-7 days at 37°C. Prior to attaining confluence, cells are washed, lysed, and stained with Hoechst 33258. Fluorescence is read on a microplate spectrofluorometer. Results are expressed as mean and standard error for the concentration of drug that inhibited growth by 50%. |
| 别名 | MK-8776, MK 8776 |
| 分子量 | 376.25 |
| 分子式 | C15H18BrN7 |
| CAS No. | 891494-63-6 |
| Smiles | Cn1cc(cn1)-c1cnn2c(N)c(Br)c(nc12)[C@@H]1CCCNC1 |
| 密度 | 1.80 g/cm3 |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 100 mg/mL (265.78 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (10.63 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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