| CAS NO: | 1431326-61-2 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 25mg | 电议 |
| 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 SMILES | NC(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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation 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: |
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