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BAY885

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纯度: 99.83%

货号 T10479Cas号 2307249-33-6

BAY885 是选择性 ERK5抑制剂,IC50为 35 nM。

BAY885
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BAY885

一键复制产品信息
Rating icon 很棒

纯度: 99.83%

货号 T10479Cas号 2307249-33-6

BAY885 是选择性 ERK5抑制剂,IC50为 35 nM。

规格价格库存数量
1 mg
¥ 737
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5 mg
¥ 1,620
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10 mg
¥ 2,690
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25 mg
¥ 4,390
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50 mg
¥ 6,220
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1 mL x 10 mM (in DMSO)
¥ 1,830
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产品介绍


BAY885 AI Summary
BAY885 demonstrates significant bioactivities related to the inhibition of specific enzymes and cellular processes. It inhibits His-tagged MAP2K5 activated ERK5 with an IC50 of 35.0 nM and ERK5 in human SN12C cells as measured by MEF2 transcription with IC50 and IC90 values of 115.0 nM and 691.0 nM, respectively. Additionally, it inhibits rat FER, human EPHB3, and human EPHA5 with inhibition rates of 62.0%, 58.0%, and 43.0%, respectively. Despite its potent enzymatic inhibition, it has low cytotoxicity against human SN12C-CMV-Luc cells (IC50 > 30000.0 nM), indicating selective targeting. BAY885 also shows varied effects on cell viability, as a growth rate of 0.0 and 1.0 was observed in HEK293T cells, U2OS cells, and human fibroblasts, suggesting complex bioactivity across different cell lines. Thermal Shift Assays reveal that BAY885 affects protein domain stability, showing both stabilizing and destabilizing effects on different regions. It exhibits high potency in targeting MAPK7 (ERK5) with an IC50 of 35.0 nM in a biochemical affinity assay and in cellular contexts, making it a significant inhibitor of the MAPK7 enzyme. However, it shows low activity against various other kinases and moderate activity against SIGMAR1. Overall, BAY885 appears to intricately influence kinase signaling pathways and cellular processes regulated by ERK5 and related enzymes..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
BAY885 is a new ERK5 inhibitor.
靶点活性
ERK5:35 nM (IC50)
化学信息
分子量515.53
分子式C25H28F3N7O2
CAS No.2307249-33-6
SmilesCN1CCN(CC1)c1cnc2c(ncnc2c1)C1CCN(CC1)C(=O)c1ccc(OC(F)(F)F)cc1N
密度1.362 g/cm3 (Predicted)
储存&溶解度
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: 16.67 mg/mL (32.34 mM), Sonication is recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (1.94 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
1mg5mg10mg50mg
1 mM1.9398 mL9.6988 mL19.3975 mL96.9876 mL
5 mM0.3880 mL1.9398 mL3.8795 mL19.3975 mL
10 mM0.1940 mL0.9699 mL1.9398 mL9.6988 mL
20 mM0.0970 mL0.4849 mL0.9699 mL4.8494 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL, 一共给药动物10只,您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH2O, 那么您的工作液浓度为2 mg/mL
母液配置方法:2 mg 药物溶于 100 μL DMSO ( 母液浓度为 20 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:100 μL DMSO 母液, 添加 400 μL PEG300 混匀澄清, 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 混匀澄清
以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
方案所需的各类助溶剂如: DMSOPEG300PEG400Tween 80SBE-β-CD玉米油等, 均可在TargetMol网站点击购买。
1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

剂量转换

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