ORY-1001 (Synonyms: Iadademstat, RG-6016) |
| カタログ番号GC11360 |
KDM1Aの選択的阻害剤。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1431326-61-2
Sample solution is provided at 25 µL, 10mM.
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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).
| Cas No. | 1431326-61-2 | SDF | |
| 同義語 | Iadademstat, RG-6016 | ||
| Chemical Name | N1-((1R,2S)-2-phenylcyclopropyl)cyclohexane-1,4-diamine | ||
| Canonical SMILES | NC(CC1)CCC1N[C@H]2[C@H](C3=CC=CC=C3)C2 | ||
| Formula | C15H24Cl2N2 | M.Wt | 303.27 |
| 溶解度 | PBS (pH 7.2): 10 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.2974 mL | 16.487 mL | 32.9739 mL |
| 5 mM | 0.6595 mL | 3.2974 mL | 6.5948 mL |
| 10 mM | 0.3297 mL | 1.6487 mL | 3.2974 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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