- p53 tumor suppressor fragment
- tumor protein p53 binding protein fragment [Homo sapiens]/[Mus musculus]
- Nutlin-3a chiral
| AMG232p53-MDM2 inhibitor, novel |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
| Description | AMG232 is a potent, selective and orally bioavailable inhibitor of MDM2−p53 interaction with IC50 value of 9.1 nM in EdU cells. | |||||
| Targets | MDM2−p53 interaction | |||||
| IC50 | 9.1 nM (in EdU cells) | |||||
| Cell experiment [1,2]: | |
Cell lines | SJSA-1, HCT116, and ACHN tumor cell lines |
Preparation method | Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 0.1, 1, or 10 μmol/L, 24 hours |
Applications | AMG 232 induced p53 signaling with an IC50 of 0.6 ± 0.4 nmol/L. AMG 232 inhibits cell proliferation in p53 WT cell lines. AMG 232 treatment inhibited the growth of cells with IC50 values ranging from 0.1 to 1 μmol/L. AMG 232 caused a dose-dependent accumulation of p53 and increased p21, MDM2, and PUMA proteins in both MDM2-amplified SJSA-1 cells and non–MDM2-amplified HCT116 cells. AMG 232 potently inhibited proliferation of non-MDM2-amplified HCT116 colorectal cells. |
| Animal experiment [1,2]: | |
Animal models | Female athymic nude mice bearing SJSA-1 cells and HCT116 cells |
Dosage form | 10 mg/kg, 25 mg/kg, 75 mg/kg; once per day by oral gavage, |
Application | AMG 232 (10 mg/kg, 25 mg/kg, 75 mg/kg, 6 hours) treatment resulted in time- and dose-dependent induction of p21 mRNA in SJSA-1 tumor. AMG 232 treatment also caused a dose-dependent induction of p21, MDM2, and PUMA mRNA in HCT116 tumors. AMG 232 (100 mg/kg, 4 days) treatment caused cell-cycle arrest and induced apoptosis in mice bearing SJSA-1 or HCT116 tumors. AMG 232 (orally once daily) enhanced the antitumor activity of DNA-damaging cytotoxics. AMG 232 displayed robust tumor growth inhibition with an ED50 of 9.1 mg/kg q.d. AMG 232 caused a dose-dependent tumor growth inhibition with an ED50 of 16 mg/kg. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Canon J, Osgood T, Olson S H, et al. The MDM2 inhibitor AMG 232 demonstrates robust anti-tumor efficacy and potentiates the activity of p53-inducing cytotoxic agents[J]. Molecular cancer therapeutics, 2015: molcanther. 0710.2014. [2]. Rew Y, Sun D. Discovery of a small molecule MDM2 inhibitor (AMG 232) for treating cancer[J]. 2014. | |
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| Cas No. | 1352066-68-2 | SDF | Download SDF |
| Synonyms | AMG 232;AMG-232 | ||
| Chemical Name | 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid | ||
| Canonical SMILES | CC(S(C[C@@H](N([C@H](C1=CC=C(Cl)C=C1)[C@@H](C2=CC=CC(Cl)=C2)C[C@]3(C)CC(O)=O)C3=O)C(C)C)(=O)=O)C | ||
| Formula | C28H35Cl2NO5S | M.Wt | 568.55 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
AMG-232 is a novel inhibitor of p53-MDM2 with IC50 value of 9.2 nM [1].
Tumor protein p53 (p53) is a very unstable protein with a half-life ranging from 5 to 30 min and participates in a variety of anticancer processes, such as inducing cell apoptosis and inhibiting angiogenesis. Mouse double minute 2 homolog (MDM2), also named as E3 ubiquitin-protein ligase Mdm2, involves in mediating p53 tumor suppressor. It has been conclusively demonstrated p53 is under-expressed in tumor cells [2].
AMG-232 is a potent p53-MDM2 interaction inhibitor and is regarded as a promising drug in clinic. When tested with SJSA-1 tumor cell line, AMG-232 treatment resulted in cell-cycle arrest and inhibition of tumor cell proliferation via binding to MDM2 protein and robustly inducing p53 activity. It was shown that p53-MDM2 bond rang from a Kd of 60 to 700 nM Depending on the length of p53 peptide [3].
In mouse model with SJSA-1 tumor cells subcutaneous xenograft, co-administration of AMG-232 and chemotherapies induced DNA damage and p53 activity which resulted in significantly superior antitumor efficacy and regression through arresting cell growth and inducting apoptosis [3].
References: [1]. Rew, Y., et al., Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction. J Med Chem, 2014. 57(24): p. 10499-511.[2]. Moll, U.M. and O. Petrenko, The MDM2-p53 interaction. Mol Cancer Res, 2003. 1(14): p. 1001-8.[3]. Canon, J., et al., The MDM2 Inhibitor AMG 232 Demonstrates Robust Antitumor Efficacy and Potentiates the Activity of p53-Inducing Cytotoxic Agents. Mol Cancer Ther, 2015. 14(3): p. 649-58.
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2、其工作原理是通过温度传感器对环境温度自动进行采样、即时监控，当环境温度高于控制设定值时控制电路启动，可以设置控制回差。如温度还在升，当升到设定的超限报警温度点时，启动超限报警功能。当被控制的温度不能得到有效的控制时，为了防止设备的毁坏还可以通过跳闸的功能来停止设备继续运行。主要应用于电力部门使用的各种高低压开关柜、干式变压器、箱式变电站及其他相关的温度使用领域。
在欧洲绝大多情况是温控器是壁挂炉必配件，两者一配一的同时交付用户的，而且配备的温控器大多是智能型温控器。而在国内，已安装在运行和正在安装调试准备投入使用的壁挂炉近95%的没有先行配备任何形式的简易或智能型的温控器。而房间采暖系统中配备温控器尤其是智能温控器，是节能采暖综合体系中一个极为突出的最重要的环节。
方便——每天自动定时提前或延后开关调节壁挂炉，免去人工操作，对上班族家庭最有必要；
舒适——每天早午晚夜各时段室温自动高低调整，免去早晨起床和下班回家后等待房间升温而挨冻的尴尬；
省气——改落后粗放的水温控制为先进准确的室温控制，加上分时段定室温按需运行，不用敞开的昼夜烧气采暖；
放心——室温过低时强制启动壁挂炉，仅需极少的燃气，便可安全的进行居室防冻保护。
温控器一般安在人多的客厅的，和办公室的空调开关一样，它是有线连接。在装修时要留一条由壁挂炉底部到客厅的暗线管，内留两根多股的胶线。
有机械式的和电子式的，
机械式的采用两层热膨胀系数不同金属压在一起，温度改变时，他的弯曲度会发生改变，当弯曲到某个程度时，接通（或断开）回路，使得制冷（或加热）设备工作。
电子式的通过热电偶、铂电阻等温度传感装置，把温度信号变换成电信号，通过单片机、PLC等电路控制继电器使得加热（或制冷）设备工作（或停止）。
还有水银温度计型的,温度到就会有触点和水银接通
请教
望版主加固本话题！
谢谢！
对不起没有没有财富值了
这里我想像大家介绍一种新的高效细胞活性和细胞增殖测定剂——alamarBlue。介绍之前先说最重要的一点，使用alamarBlue价格比较昂贵，如果你的银子不多，呵呵，还是乖乖告诉老板你的MTT结果吧。
细胞增殖检测主要有三种方法：第一、增殖期抗体的测定（例如Ki-67和CydlinE）。第二、增殖期DNA合成标记（3H,BrdU等）。相信这两种方法少有人做，反正以前我都没听过（见笑了）。还有第三就是增殖细胞对外界环境物质的降解测定（包括大家常做的MTT和XTT、MTS，还有今天要介绍的AlamarBlue）。
AlamarBlue是一种新型的细胞活性和细胞增殖的指示剂，是一种可溶、稳定、无毒的靛蓝染料，同时适用于贴壁和悬浮细胞。它对细胞抗原的表达和杂交瘤细胞的抗体分泌功能无影响，而且非常有意义的一点就是，经过AlamarBlue测定的细胞可以继续培养或进行其他的功能测定。AlamarBlue可以用普通分光光度计、荧光光度计和酶标仪进行测定，非常方便，其测定结果同样有线性趋势，而且线性范围更广，更灵敏和稳定。
主要应用于：
a.优化细胞培养条件
b.对细胞生长因子或细胞因子进行活性定量
c.有助于开发抗生素或抗肿瘤的新药
d.了解毒性物质或污染物对细胞生长的影响
e.评估细胞介导的细胞毒作用
f.定量检测凋亡发生
g.适用于真核细胞、真菌和细菌的活性和增殖测定。
附件是AlamarBlue的产品详细说明，实验操作手册。感兴趣的战友可以看一看。还有一篇文章是比较MTT和AlamarBlue的，不过很遗憾，我没能查到全文，如果哪位高手能查出来，真心希望能够贴出来与大家分享。
Hamid,R.,Rotshteyn,Y.,RabADI,L.etal.ComparisonofalamarblueandMTTassaysforhighthrough-putscreening.ToxicologyinVitro.200418(5);703-710.
alamarbluebooklet.pdf(153.16k)
