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SCH900776
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SCH900776图片
CAS NO:891494-63-6
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
50 mg电议
100 mg电议

产品名称
MK 8776
MK-8776
产品介绍
SCH900776 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。

产品描述

CHK1 Inhibitor MK-8776 is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities.

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%.

Cas No.

891494-63-6

分子式

C15H18BrN7

分子量

376.25

别名

MK 8776;MK-8776

储存和溶解度

DMSO:100 mg/mL (265.78 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years