ORY-1001 free base

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MedKoo CAT#: 527485

CAS#: 1431304-21-0 (free base)

Description: ORY1001, also known as RG-6016, is KDM1A inhibitor (IC50 <20nM) with high selectivity against related FAD dependent aminoxidases (MAO-A/B, IL4I1, KDM1B >100uM, SMOX 7uM). ORY-1001 does not inhibit non-related histone modifiers. Treatment of THP-1 (MLL-AF9) cells with ORY-1001, results in a time/dose dependent me2H3K4 accumulation at KDM1A target genes and concomitant induction of differentiation markers (EC50 me2H3K4 and FACS CD11b <1nM). ORY-1001 induces apoptosis in THP-1 and inhibits proliferation and colony formation of MV(4;11) (MLL-AF4) cells (EC50 <1nM).

Chemical Structure

ORY-1001 free base
CAS# 1431304-21-0 (free base)

Theoretical Analysis

MedKoo Cat#: 527485
Name: ORY-1001 free base
CAS#: 1431304-21-0 (free base)
Chemical Formula: C15H22N2
Exact Mass: 230.1783
Molecular Weight: 230.355
Elemental Analysis: C, 78.21; H, 9.63; N, 12.16

Price and Availability

Size Price Availability Quantity
5.0mg USD 295.0 2 Weeks
10.0mg USD 485.0 2 Weeks
25.0mg USD 865.0 2 Weeks
50.0mg USD 1305.0 2 Weeks
100.0mg USD 2250.0 2 Weeks
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Related CAS #: 1431303-72-8 (2HCl)   1431304-21-0 (free base)   1431303-71-7 (xHCl)   1431326-61-2 (2HCl)  

Synonym: ORY-1001; ORY1001; ORY 1001; RG6016; RG 6016; RG-6016

IUPAC/Chemical Name: N-[(1R,2S)-2-Phenylcyclopropyl]-1,4-cyclohexanediamine

InChi Key: NC1CCC(N[C@H]2[C@H](C3=CC=CC=C3)C2)CC1

InChi Code: InChI=1S/C15H22N2/c16-12-6-8-13(9-7-12)17-15-10-14(15)11-4-2-1-3-5-11/h1-5,12-15,17H,6-10,16H2/t12?,13?,14-,15+/m0/s1


Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 230.355 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Hosseini A, Minucci S. A comprehensive review of lysine-specific demethylase 1 and its roles in cancer. Epigenomics. 2017 Aug;9(8):1123-1142. doi: 10.2217/epi-2017-0022. Epub 2017 Jul 12. PubMed PMID: 28699367.

2: Zheng YC, Yu B, Jiang GZ, Feng XJ, He PX, Chu XY, Zhao W, Liu HM. Irreversible LSD1 Inhibitors: Application of Tranylcypromine and Its Derivatives in Cancer Treatment. Curr Top Med Chem. 2016;16(19):2179-88. Review. PubMed PMID: 26881714.

3: Maes T, Mascaró C, Ortega A, Lunardi S, Ciceri F, Somervaille TC, Buesa C. KDM1 histone lysine demethylases as targets for treatments of oncological and neurodegenerative disease. Epigenomics. 2015;7(4):609-26. doi: 10.2217/epi.15.9. Review. PubMed PMID: 26111032.