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ORY-1001
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ORY-1001图片
CAS NO:1431326-61-2
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
25mg电议

产品介绍
Selective inhibitor of KDM1A.
Cas No.1431326-61-2
别名N1-(反式-2-苯基环丙基)环己烷-1,4-二胺二盐酸盐
化学名N1-((1R,2S)-2-phenylcyclopropyl)cyclohexane-1,4-diamine
Canonical SMILESNC(CC1)CCC1N[C@H]2[C@H](C3=CC=CC=C3)C2
分子式C15H24Cl2N2
分子量303.27
溶解度PBS (pH 7.2): 10 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50:<20nM

Lysine (K)-specific demethylase 1A (KDM1A, aka LSD1) is a key regulator of leukemia stem cell (LSC) potential and is required for MLL-AF9 oncogenic transformation. Inhibition of KDM1A expression or activity overcomes the differentiation block in AML. ORY-1001 is a selective inhibitor of KDM1A.

In vitro: ORY-1001 is an enantiomerically pure KDM1A inhibitor with high selectivity against related FAD dependent aminoxidases. ORY-1001 does not inhibit non-related histone modifiers, and is clean in a CEREP diversity panel. Treatment of THP-1 cells with ORY-1001, results in a time/dose dependent me2H3K4 accumulation at KDM1A target genes and concomitant induction of differentiation markers [1].

In vivo: Daily oral administration of doses< 0.020 mg/kg leads to significantly reduced tumor growth in rodent xenografts. In vivo studies have shown that ORY-1001 presents excellent oral bioavailability, target exposure and activity in vivo [1].

Clinical trial: Oryzon Genomics announced the dosing of the first patient in the extension cohort (Part 2) of its ORY-1001 Phase I clinical trial. The trial will take place in 10 centers in Spain, UK and France.

Reference:
[1] Tamara Maes, I?igo 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).