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]恶嗪盐酸盐 CAS#: 600734-06-3

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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]恶嗪盐酸盐

生物活性靶点体外研究体内研究 用途与合成方法 MSDS 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]恶嗪盐酸盐价格(试剂级) 上下游产品信息

中文名称	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]恶嗪盐酸盐
中文同义词	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]恶嗪盐酸盐;化合物 T14508;化合物 BAY 65-1942 HYDROCHLORIDE
英文名称	7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one hydrochloride
英文同义词	Bay 65-1942 (HCl salt);Bay 65-1942 HCl;Bay 65-1942 (hydrochloride);(S)-7-(2-(cyclopropylmethoxy)-6-hydroxyphenyl)-5-(piperidin-3-yl)-1H-pyrido[2,3-d][1,3]oxazin-2(4H)-one hydrochloride;7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one hydrochloride;KINK-1 hydrochloride;KINK-1 hydrochloride >=98% (HPLC);2H-Pyrido[2,3-d][1,3]oxazin-2-one,7-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-,Hydrochloride(1:1)
CAS号	600734-06-3
分子式	C22H25N3O4.ClH
分子量	431.917
EINECS号
相关类别
Mol文件	600734-06-3.mol
结构式

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]恶嗪盐酸盐 性质

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]恶嗪盐酸盐 用途与合成方法

生物活性

Bay 65-1942 hydrochloride 是一种 ATP 竞争性的选择性 IKKβ 抑制剂。

靶点

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 IC     ₅₀    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 IC     ₇₅    (CI = 0.48±0.01). Synergism is also indicated at the IC     ₅₀    (CI = 0.56±0.09) and IC     ₉₀    (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.

安全信息

MSDS信息

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]恶嗪盐酸盐 价格(试剂级)

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]恶嗪盐酸盐 上下游产品信息