| 中文名称: | Bay 65-1942 free base | ||||
|---|---|---|---|---|---|
| 英文名称: | Bay 65-1942 free base | ||||
| 别名: | 7-[2-(环丙基甲氧基)-6-羟基苯基]-1,4-二氢-5-(3S)-3-哌啶基-2H-吡啶并[2,3-d][1,3]恶嗪-2-酮;7-[2-(环丙基甲氧基)-6-羟基苯基]-1,4-二氢-5-(3s)-3-哌啶基-2H-吡啶并[2,3-d][1,3]噁嗪-2-酮;Bay 65-1942 (游离基) 7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one | ||||
| CAS No: | 600734-02-9 | 分子式: | C22H25N3O4 | 分子量: | 395.45 |
| CAS No: | 600734-02-9 | ||||
| 分子式: | C22H25N3O4 | ||||
| 分子量: | 395.45 | ||||
包装规格：
5mg in glass bottle
产品简介：
一种ATP竞争性的选择性IKKβ抑制剂。
靶点：
IKKβ
体外研究：
Delivery of Bay 65-1942 prior to ischemia significantly decreases left ventricular infarct size compared with animals receiving vehicle. Compared with sham animals, animals receiving vehicle have a significant increase in the infarct-to-area at risk (AAR) ratio (70.7±3.4 vs. 5.8±3.4%, P<0.05). This ratio is significantly reduced by treatment with Bay 65-1942 at each time point (prior to ischemia 42.7±4.1%, at reperfusion 42.7±7.5%, 2 h of reperfusion 29.4±5.2%; each group P<0.05 vs. vehicle). Animals pretreated with Bay 65-1942 (n=3) have significantly attenuated CK-MB levels compared with those animals without treatment prior to IR (14,170 ±3,219 units, P<0.05 vs. vehicle).
体内研究：
Inhibitors of MEK (AZD6244) and IKK (BAY 65-1942) are used at their IC50 concentrations, as determined by a 48 hour MTS assay, which achieve sufficient inhibition of kinase activity. MYL-R cells are treated for 24 hours with AZD6244 (5 µM), BAY 65-1942 (10 µM), or a combination of these inhibitors at the same concentrations. AZD6244 and BAY 65-1942 demonstrate synergistic inhibition of cell viability at the dose combination (5 µM AZD6244+10 µM BAY 65-1942), which correlates with IC75 (CI = 0.48±0.01). Synergism is also indicated at the IC50 (CI = 0.56±0.09) and IC90 (CI = 0.46±0.02) dose combinations reported by the software (CI values are the mean of three independent experiments, ± standard deviation). AZD6244 and BAY 65-1942 treatment induces 2- and 1.3-fold caspase 3/7 activation, respectively, compared to the DMSO-treated cells. Treatment with a combination of AZD6244 plus BAY 65-1942 leads to a 3.2-fold increase in caspase 3/7 activity.
保存条件：
-20℃
注意事项：
1、为了您的安全和健康，请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
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安全说明：
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参考文献 & 客户发表文献
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