ORY-1001
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.
IC50: 小于20 nM.
赖氨酸(K)特异性去甲基酶1A简称KDM1A,又名LSD1,是白血病干细胞(LSC)潜力的关键调节剂,对于MLL-AF9的恶性转化是必须的.抑制KDM1A的表达或活性克服了AML的分化阻断.ORY-1001是KDM1A的选择性抑制剂.
体外实验:ORY-1001是对映体纯KDM1A抑制剂,对相关的FAD依赖性氨氧化酶具有高选择性.ORY-1001不抑制不相关的组蛋白修饰剂.使用ORY-1001处理THP-1细胞,以时间和剂量依赖性的方式引起me2H3K4在KDM1A靶基因上的积累,并伴随诱导分化标记物[1].
在体实验:在啮齿动物异种移植模型中,每日口服给药剂量小于0.020 mg/kg 的ORY-1001显著减少肿瘤生长.体内研究表明,ORY-1001具有较好的口服生物利用度\靶向曝露和体内活性[1].
临床试验:Oryzon华大基因宣布了ORY-1001的I期临床试验中扩展队列 (Part 2)在第一个病人中的剂量.该试验将在西班牙\英国和法国的10个中心进行.
参考文献：
[1] Tamara Maes, Iigo Tirapu, Cristina Mascaró, Alberto Ortega, Angels Estiarte, Nuria Valls, Julio Castro-Palomino, Carlos Buesa Arjol, Guido Kurz; Oryzon Genomics, S. A., Cornella de Llobregat. Preclinical characterization of a potent and selective inhibitor of the histone demethylase KDM1A for MLL leukemia. J Clin Oncol 31, 2013 (suppl; abstr e13543).
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 303.27 |
| Cas No. | 1431326-61-2 |
| Formula | C15H24Cl2N2 |
| Solubility | insoluble in EtOH; ≥23.15 mg/mL in H2O; ≥6.9 mg/mL in DMSO with gentle warming |
| Chemical Name | N1-((1R,2S)-2-phenylcyclopropyl)cyclohexane-1,4-diamine |
| SDF | Download SDF |
| Canonical SMILES | NC(CC1)CCC1N[C@H]2[C@H](C3=CC=CC=C3)C2 |
| 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
相关生物数据
