NMS-E973
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
NMS-E973是热休克蛋白90(Hsp90)高效选择性抑制剂,DC50值小于10 nM [1].
由于Hsp90在一些致癌蛋白的构象成熟\稳定和功能中发挥重要作用,因此Hsp90抑制剂被开发用于治疗癌症.NMS-E973是选择性Hsp90抑制剂.其结合Hsp90α的ATP结合位点,DC50值小于10 nM.此外,NMS-E973对52种不同蛋白激酶没有效应,如ABL\ACK1\AKT1和Alk.其对Hsc70的IC50值大于10 μM.
NMS-E973对A2780肿瘤细胞系和BT-474乳腺癌细胞系表现出抗增殖效应,IC50值分别为69 nM和110 nM.
在A2780异种移植的小鼠模型中,按30 mg/kg的剂量静脉内给予NMS-E973能显著抑制肿瘤生长,TGI值为53%.而且,在激酶抑制剂如vemurafenib耐受性肿瘤中,NMS-E973也具有抗肿瘤活性[1, 2].
参考文献：
[1] Brasca M G, Mantegani S, Amboldi N, et al. Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90). Bioorganic & medicinal chemistry, 2013, 21(22): 7047-7063.
[2] Fogliatto G, Gianellini L, Brasca M G, et al. NMS-E973, a novel synthetic inhibitor of Hsp90 with activity against multiple models of drug resistance to targeted agents, including intracranial metastases. Clinical Cancer Research, 2013, 19(13): 3520-3532.
| Storage | Store at -20°C |
| M.Wt | 454.43 |
| Cas No. | 1253584-84-7 |
| Formula | C22H22N4O7 |
| Solubility | Soluble in DMSO |
| SDF | Download SDF |
| Canonical SMILES | CN1CCC(CC1)NC(=O)C2=CC(=C3C(=CC(=O)C=C3OC4=CC=C(C=C4)[N+](=O)[O-])O)ON2 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | NMS-E973是高效选择性Hsp90抑制剂. | |||||
| 靶点 | Hsp90 | |||||
| IC50 | ||||||
化学结构
