| AG 825Selective ErbB2 inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
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| Cas No. | 149092-50-2 | SDF | Download SDF |
| Chemical Name | (E)-3-(3-((benzo[d]thiazol-2-ylthio)methyl)-4-hydroxy-5-methoxyphenyl)-2-cyanoacrylamide | ||
| Canonical SMILES | OC(C(CSC1=NC2=CC=CC=C2S1)=CC(/C=C(C#N)/C(N)=O)=C3)=C3OC | ||
| Formula | C19H15N3O3S2 | M.Wt | 397.47 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | 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. | ||
AG 825 is a selective inhibitor of ErbB2 with IC50 values of 0.15 and 19 μM for ErbB2 and ErbB1 respectively [1].
Receptor tyrosine-protein kinase erbB-2 is a member of the human epidermal growth factor receptor family and promotes cell proliferation.
AG 825 is a selective ErbB2 inhibitor. AG825 inhibited autophosphorylation of HER2, HER1-2 and HER1 with IC50 values of 0.15, 0.35 and 19 μM, respectively [1]. In non-small cell lung cancer (NSCLC) cell lines expressing high-p185neu, the HER-2/neu gene product, AG825 significantly increased the chemosensitivities. However, AG825 with high concentrations inhibited the drug-induced G2 arrest and the activation of phosphorylated p34cdc2 [2]. In androgen-independent prostate cancer (PCa) cell lines C4 and C4-2, AG825 was toxic in a dose- and time-dependent way and inhibited phosphoactivation of HER-2/neu and its down-regulation. Also, AG825 induced an imbalance between p38 mitogen-activated protein kinase activation and extracellular signal-regulated kinase 1/2, which then led to p38-dependent apoptosis [3].
References:[1]. Osherov N, Gazit A, Gilon C, et al. Selective inhibition of the epidermal growth factor and HER2/neu receptors by tyrphostins. J Biol Chem, 1993, 268(15): 11134-11142.[2]. Tsai CM, Levitzki A, Wu LH, et al. Enhancement of chemosensitivity by tyrphostin AG825 in high-p185(neu) expressing non-small cell lung cancer cells. Cancer Res, 1996, 56(5): 1068-1074.[3]. Murillo H, Schmidt LJ, Tindall DJ. Tyrphostin AG825 triggers p38 mitogen-activated protein kinase-dependent apoptosis in androgen-independent prostate cancer cells C4 and C4-2. Cancer Res, 2001, 61(20): 7408-7412.
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最好添上出处，谢谢各位！
1、在实验室内一切有可能产生毒性蒸气的工作必须在通风橱中进行，并有良好的排风设备。2、在稀释浓硫酸时，不能将水往浓硫酸里倒，而应将浓硫酸缓缓倒入水中，不断搅拌均匀。3、取用有毒、有恶臭味的试剂时，要在通风橱中操作；使用完毕后，将瓶口封严。4、化学危险物品应当分类、分项存放，还原性试剂与氧化剂、酸与碱类腐蚀剂等不得混放，相互之间保持安全距离。5、受阳光照射易燃烧、易爆炸或产生有毒气体的化学危险品应当在阴凉通风的地点存放。
