AZD3264
目录号 : GC10135
An inhibitor of IKK2
Cas No.:1609281-86-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Target: IKK2
IC50: N/A
AZD3264 is a novel and small molecule IKK2 inhibitor.
IKK2 serves as a protein subunit of IκB kinase, which is a component of the cytokine-activated intracellular signaling pathway involved in triggering immune responses. IKK's activity induces the activation of a transcription factor NF-κB. Activated IKK2 phosphorylates IκB (IκBα), which binds NF-κB to inhibit its function. Phosphorylated IκB is degraded by the ubiquitination pathway, freeing NF-κB, and allowing its entry into the cell nucleus where it activates target genes involved in inflammation and other immune responses. Suppression of IKK2 has been identified as a potential therapeutic option to treat cancer and inflammatory diseases, including asthma, chronic pulmonary obstructive disorder (COPD) and rheumatoid arthritis [1].
In vitro: AZD3264, by inhibiting IKK2, was currently in preclinical development for the potential treatment of inflammatory diseases such as asthma, chronic pulmonary obstructive disorder (COPD) and rheumatoid arthritis [2].
In vivo: N/A
References:
1. Llona-Minguez S, Baiget J, Mackay SP. Small-molecule inhibitors of IkappaB kinase (IKK) and IKK-related kinases. Pharm Pat Anal. 2013;2(4):481-98.
2. Murugan A, et al. Org. Process Res. Dev. 2014, 18, 646-651.
Cas No. | 1609281-86-8 | SDF | |
化学名 | (S)-5-(4-(3,5-dimethylisoxazol-4-yl)-2-(pyrrolidin-3-yloxy)phenyl)-2-ureidothiophene-3-carboxamide | ||
Canonical SMILES | CC1=NOC(C)=C1C2=CC(O[C@H]3CCNC3)=C(C4=CC(C(N)=O)=C(NC(N)=O)S4)C=C2 | ||
分子式 | C21H23N5O4S | 分子量 | 441.5 |
溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml | 储存条件 | Store at -20°C |
General tips | 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。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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1 mg | 5 mg | 10 mg |
1 mM | 2.265 mL | 11.325 mL | 22.6501 mL |
5 mM | 0.453 mL | 2.265 mL | 4.53 mL |
10 mM | 0.2265 mL | 1.1325 mL | 2.265 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。