|N1-(反式-2-苯基环丙基)环己烷-1,4-二胺二盐酸盐|CsnPharm

CAS No.: 1431326-61-2

trans-N1-(2-Phenylcyclopropyl)cyclohexane-1,4-diamine dihydrochloride Catalog No. CSN16347

Synonyms: Iadademstat;RG-6016

ORY-1001 is a selective inhibitor of lysine-specific demethylase LSD1/KDM1A with IC50 of < 20 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 KDM1A

IC50:20nM
描述ORY-1001 is a highly potent and selective KDM1A inhibitor with IC50 value of 18nM. It engaged enzymatically active KDM1A in THP1 cells with an EC50 of 0.63nM and 0.55 nM after 24 and 96 hr of treatment, respectively. Inhibition of KDM1A by ORY-1001 induced H3K4me2 accumulation on KDM1A target genes. The ten genes that were most potently induced after 96 hr were VCAN, S100A8, S100A9, S100A12, LYZ, ANXA2, ANXA8, OSBPL11, KCKN13, and FCRLA. Genes significantly downregulated by ORY-1001 include genes de-regulated in MLL-translocated AML (CCL5, RHOBTB3, HOXA9, HOXA10, HOXA11) as well as genes identified as direct targets of MLL-AF9 or MLL-AF4 (HOXA10, CDK6, SLC38A1, HIVEP2, ARHGAP25, TAPT1, REEP3, PPP3R2, and FLT3) and KIT. ORY-1001 potently reduced the colony-forming potential in a variety of AML cell lines, with MLL-translocated AML cell lines such as THP1 (MLL-AF9) and MV(4;11) (MLL-AF4) being the most sensitive, and induced blast differentiation, and reduction of leukemic stem cell capacity in AML. ORY-1001 exhibited potent synergy with standard-of-care drugs and selective epigenetic inhibitors, reduced growth of an AML xenograft model, and extends survival in a mouse PDX model of T cell acute leukemia at dose of 0.0125mg/kg^[2].
作用机制ORY-1001 could rapidly and covalently bind to the FAD cofactor in KDM1A in a manner analogous to tranylcypromine.^[2]
动物研究
剂量
Mice: 0.02 mg/kg^[1] (o.g.); 0.0125 mg/kg^[1] (i.p.)

给药途径
o.g., i.p.
参考文献

动物研究
剂量	Mice: 0.02 mg/kg^[1] (o.g.); 0.0125 mg/kg^[1] (i.p.)
给药途径	o.g., i.p.

[1] Maes T, Mascaró C, et al. ORY-1001, a Potent and Selective Covalent KDM1A Inhibitor, for the Treatment of Acute Leukemia. Cancer Cell. 2018 Mar 12;33(3):495-511.e12.
[2] Maes T, Mascaró C, Tirapu I, Estiarte A, Ciceri F, Lunardi S, Guibourt N, Perdones A, Lufino MMP, Somervaille TCP, Wiseman DH, Duy C, Melnick A, Willekens C, Ortega A, Martinell M, Valls N, Kurz G, Fyfe M, Castro-Palomino JC, Buesa C. ORY-1001, a Potent and Selective Covalent KDM1A Inhibitor, for the Treatment of Acute Leukemia. Cancer Cell. 2018 Mar 12;33(3):495-511.e12. doi: 10.1016/j.ccell.2018.02.002. Epub 2018 Mar 1. PMID: 29502954.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.2974 mL
- 16.4869 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

技术信息

CAS号

1431326-61-2

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H24Cl2N2

运输

蓝冰

分子量

303.27

别名

Iadademstat;RG-6016

溶解度

DMSO	5.0 mg/mL (16.5 mM)
Ethanol	4.0 mg/mL (13.2 mM) warming

动物实验配方

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trans-N1-(2-Phenylcyclopropyl)cyclohexane-1,4-diamine dihydrochloride Catalog No. CSN16347

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