Exemestane
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.
Exemestane(依西美坦)是一种新型不可逆的芳香化酶选择性抑制剂,IC50值为27 nM。Exemestane对人胎盘芳香化酶的Ki值为26 nM,t1 / 2为13.9 min[1]。
芳香化酶是一种细胞色素P450酶,催化雄激素到雌激素的转化[2]。结构上与雄烯二酮类似,Exemestane对雄激素的效应具有很大的影响。Exemestane可与芳香化酶肽部分的底物结合位点相互作用,造成不可逆的芳香化酶失活。结合于活性位点后,它可转换为一个中间物质,与芳香化酶结合位点共价结合,使酶失去活性。Exemestane可以抑制体外人胎盘微粒体的芳香酶活性,此外,它可以抑制培养的组织成纤维细胞和乳腺癌标本的芳香化酶活性。另一方面,Exemestane可影响体内血液水平和尿雌激素 [3]。
参考文献:
[1] Franco Buzzetti, Enrico Di Salle, Antonio Longo, Gabriella Briatico. Synthesis and aromatase inhibition by potential metabolites of exemestane (6-methylenandrosta-1,4-diene-3,17-dione). Steroids. November 1993. 58(11): 527-532.
[2] Gustavo de Albuquerque Cavalcanti, Bruno Carius Garrido, Felipe Dias Leal, Monica Costa Padilha, Xavier de la Torre, Francisco Radler de Aquino Neto. Detection of new urinary exemestane metabolites by gas chromatography coupled to mass spectrometry. Steroids. September–October 2011. 76(10-11): 1010-1015.
[3] Stephanie A. Jones, Stephen E. Jones. Exemestane: A Novel Aromatase Inactivator for Breast Cancer. Clinical Breast Cancer. October 2000. 1(3): 211-216.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 296.4 |
Cas No. | 107868-30-4 |
Formula | C20H24O2 |
Solubility | insoluble in H2O; ≥14.82 mg/mL in DMSO; ≥15.23 mg/mL in EtOH |
Chemical Name | (8R,9S,10R,13S,14S)-10,13-dimethyl-6-methylidene-7,8,9,11,12,14,15,16-octahydrocyclopenta[a]phenanthrene-3,17-dione |
SDF | Download SDF |
Canonical SMILES | CC12CCC3C(C1CCC2=O)CC(=C)C4=CC(=O)C=CC34C |
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
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