中文名称: Bay 65-1942 free base
英文名称: Bay 65-1942 free base
CAS No: 600734-02-9
分子式: C22H25N3O4
分子量: 395.45
B11706 Bay 65-1942 free base (psaitong)
包装规格:
5mg in glass bottle
产品描述:

基本信息

产品编号:

B11706

产品名称:

Bay 65-1942 free base

CAS:

600734-02-9

 

储存条件

粉末

-20℃

四年

分子式:

C22H25N3O4

溶于液体

-80℃

四年

分子量:

395.45

 

 

化学名: 

7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one

Solubility (25°C):

 

体外:

 

DMSO

 

Ethanol

 

Water

 

体内(现配现用):

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。

 

生物活性

产品描述

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%,2h of reperfusion 29.4±5.2%;each group P<0.05vs.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 (5µM),BAY 65-1942 (10µM),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 (5µM AZD6244+10µM 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.

 

推荐实验方法(仅供参考)

细胞实验:

 

Cell viability is determined by seeding MYL-R cells on a 96-well plate at 4×104 cells/well in 100µL RPMI growth medium supplemented with kinase inhibitors.Growth media and kinase inhibitors are replenished at 24 hours,and at 48 hours.20µL of MTS assay reagent is added to each well.The plate is returned to the incubator for approximately 1 hour and the absorbance at 490nm is recorded.For combination index (CI) experiments,cells are grown and assayed.To determine AZD6244 and BAY 65-1942 (10µM) dose-effects,cells are treated with a series of three-fold dilutions of each drug singly,or in combination while maintaining a constant ratio of 1:2,respectively.Cell viability results are analyzed to derive CI values.The CI values from three independent experiments are averaged.

 

动物实验:

 

Mice

Male C57BL/6 mice,8-10 wk of age are used.To investigate IKKβ inhibition in myocardial IR injury,mice are subjected to 30 min of cardiac ischemia followed by varying periods of reperfusion.An intraperitoneal injection of Bay 65-1942 (5mg/kg) at appropriate dosing time points is administered.Nontreatment groups receive a vehicle of 10% cremaphor in water.In treatment groups,Bay 65-1942 is delivered either prior to ischemia,at the time of reperfusion,or 2h after reperfusion injury.Infarct size is measured 24h after reperfusion injury in sham,vehicle,and each treatment group.To confirm myocardial injury,serum creatine kinase-muscle-brain fraction (CK-MB) levels are measured 1h after reperfusion in animals pretreated with Bay 65-1942. 

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
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摩尔浓度计算公式

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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):