ENMD-2076 L-(+)-Tartaric acid
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.
ENMD-2076是一种口服生物可利用的小分子Aurora激酶抑制剂，对Aurora激酶A和Aurora激酶B的IC50值分别为14 nM和350 nM。
除Aurora激酶外，ENMD-2076可抑制参与多种细胞活动的激酶。由于在乳腺癌中发现Aurora激酶A的过表达，ENMD-2076被用于乳腺癌研究。据报道ENMD-2076可不同程度地抑制29种乳腺癌细胞系，IC50值从0.25到16.1 μM不等。在克隆形成试验中，ENMD-2076可完全抑制敏感型MDA-MB-468细胞系的集落形成，并能降低HCC1806、K-BR-3和BT474细胞系的集落形成。ENMD-2076在1.25 μM下也可导致G2细胞周期停滞。此外，ENMD-2076在TNBC异种移植模型中具有抗癌活性。除乳腺癌外，ENMD-2076被研究用于恶性血液病治疗。已有II期临床试验进行[1,2]。
参考文献：
[1] Diamond JR, Eckhardt SG, Tan AC, Newton TP, Selby HM, Brunkow KL, Kachaeva MI, Varella-Garcia M, Pitts TM, Bray MR, Fletcher GC, Tentler JJ. Predictive biomarkers of sensitivity to the aurora and angiogenic kinase inhibitor ENMD-2076 in preclinical breast cancer models. Clin Cancer Res. 2013 Jan 1;19(1):291-303.
[2] How J, Yee K. ENMD-2076 for hematological malignancies. Expert Opin Investig Drugs. 2012 May;21(5):717-32.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 525.56 |
| Cas No. | 1291074-87-7 |
| Formula | C25H31N7O6 |
| Solubility | insoluble in EtOH; ≥175.8 mg/mL in DMSO |
| Chemical Name | (E)-N-(5-methyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-styrylpyrimidin-4-amine 2,3-dihydroxysuccinate |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC(=NN1)NC2=NC(=NC(=C2)N3CCN(CC3)C)C=CC4=CC=CC=C4.C(C(C(=O)O)O)(C(=O)O)O |
| 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。 |
质量控制和MSDS
- 批次:
化学结构
