MK-2866 (GTx-024)
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
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Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
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Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
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Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
GTx-024[1]是一种选择性的非甾体类雄激素受体(AR)调节剂[2],在MDA-MB-231细胞中,GTx-024作用于雄激素受体的反式激活[3],EC50值为1 nM[4]。
ARs与雄激素共同负责雄性生殖系统的维持和发展。ARs也与人类的行为和前列腺癌相关[3]。
在表达AR的MDA-MB-231细胞中,GTx-024具有抗增殖效应。对于MDA-MB-231细胞的生长,GTx-024的IC50值为77±16 nM。在乳腺癌细胞中,GTx-024同时具有抗增殖效应和激动效应。这表明,MDA-MB-231-AR细胞中高效的雄激素也可忍受GTx-024强烈的抗增殖效应[4]。
与对照相比,GTx-024(3 mg)以剂量依赖的方式显著增加受试者的总瘦体重(P <0.001),导致平均瘦体重为1.3 kg±0.3(±1 SE)。在相同剂量下,总脂肪量显著(P= 0.049)减少。该剂量在脂肪量上不能区分男性群体和女性群体,与对照相比,两者均有约0.6 kg的脂肪量损失。该剂量不会影响总体重,但引起血糖和血中胰岛素的显著降低(P= 0.006)。在1 mg 和3 mg剂量时,GTx-024降低胰岛素的耐受性[2]。
参考文献:
[1]. Scarlet F. Encina. The Prevalence of Cancer Cachexia Using Different Diagnostic Criteria [D]. Florida: Florida State University, 2014.
[2]. James T. Dalton, Kester G. Barnette, Casey E. Bohl, et al. The selective androgen receptor modulator GTx-024 (enobosarm) improves lean body mass and physical function in healthy elderly men and postmenopausal women: results of a double-blind, placebo-controlled phase II trial. J Cachexia Sarcopenia Muscle, 2011, 2(3):153-161.
[3]. Hideyuki Ito, Tanya Langenhorst, Rob Ogden, et al. Androgen receptor gene polymorphism in zebra species. Meta Gene, 2015, 5:120-123.
[4]. Ramesh Narayanan, Sunjoo Ahn, Misty D. Cheney, et al. Selective Androgen Receptor Modulators (SARMs) Negatively Regulate Triple-Negative Breast Cancer Growth and Epithelial:Mesenchymal Stem Cell Signaling. PLOS ONE, 2014, 9(7):e103202.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 389.33 |
Cas No. | 841205-47-8 |
Formula | C19H14F3N3O3 |
Solubility | insoluble in H2O; ≥10.7 mg/mL in DMSO; ≥5.65 mg/mL in EtOH |
Chemical Name | (2S)-3-(4-cyanophenoxy)-N-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide |
SDF | Download SDF |
Canonical SMILES | CC(COC1=CC=C(C=C1)C#N)(C(=O)NC2=CC(=C(C=C2)C#N)C(F)(F)F)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。 |
Description | MK-2866是雄激素受体(AR)调节剂,ED50值为0.44 mg/day。 | |||||
靶点 | androgen receptor | |||||
IC50 | 0.44 mg/day (ED50) |
质量控制和MSDS
- 批次:
化学结构
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