Iadademstat (ORY-1001) 2HCl

製品コードS7795 バッチS779501

印刷

化学情報

Synonyms

RG-6016

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₅H₂₂N₂. 2HCl

分子量

303.27

CAS No.

1431326-61-2

Solubility (25°C)*

体外

Water

61 mg/mL (201.14 mM)

DMSO

5 mg/mL (16.48 mM)

Ethanol (warmed with 50ºC water bath)

4 mg/mL (13.18 mM)

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Iadademstat 2HCl (ORY-1001, RG-6016) is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor with IC50 of <20 nM, with high selectivity against related FAD dependent aminoxidases. Phase 1.
in vitro	In THP-1 (MLL-AF9) cells, ORY-1001 results in a time/dose dependent me2H3K4 accumulation at KDM1A target genes and concomitant induction of differentiation markers. ORY-1001 also induces apoptosis in THP-1 and inhibits proliferation and colony formation of MV(4;11) (MLL-AF4) cells. ^[1]
in vivo	In rodent MV(4;11) xenografts, ORY-1001 (<0.020mg/kg, p.o.) leads to significantly reduced tumor growth. ^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	NRK-52E cells
	濃度	10 μM
	反応時間	24 h
	実験の流れ	Cells treated with ORY-1001 (10 μM) for 24 h in the presence (vehicle) or TGF-β1.
動物実験	動物モデル	Rodent MV(4;11) xenografts
	投薬量	<0.020mg/kg
	投与方法	p.o.

参考

http://meetinglibrary.asco.org/content/116240-132
https://pubmed.ncbi.nlm.nih.gov/34958158/

カスタマーフィードバック

: Data from [Data independently produced by , , Br J Haematol, 2017, doi: 10.1111/bjh.14983]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A CRISPR-Cas9 screen reveals genetic determinants of the cellular response to decitabine [ EMBO Rep, 2025, 10.1038/s44319-025-00385-w]	PubMed: 39930152
Transposable elements-mediated recruitment of KDM1A epigenetically silences HNF4A expression to promote hepatocellular carcinoma [ Nat Commun, 2024, 15(1):5631]	PubMed: 38965210
Potential role of lipophagy impairment for anticancer effects of glycolysis-suppressed pancreatic ductal adenocarcinoma cells [ Cell Death Discov, 2024, 10(1):166]	PubMed: 38580661
[ORY-1001 inhibits glioblastoma cell growth by downregulating the Notch/HES1 pathway via suppressing lysine-specific demethylase 1 expression] [ Nan Fang Yi Ke Da Xue Xue Bao, 2024, 44(8):1620-1630]	PubMed: 39276059
MAF amplification licenses ERα through epigenetic remodelling to drive breast cancer metastasis [ Nat Cell Biol, 2023, 10.1038/s41556-023-01281-y]	PubMed: 37945904
Pharmacological inhibition of LSD1 suppresses growth of hepatocellular carcinoma by inducing GADD45B [ MedComm (2020), 2023, 4(3):e269]	PubMed: 37250145
E3 ligase Trim35 inhibits LSD1 demethylase activity through K63-linked ubiquitination and enhances anti-tumor immunity in NSCLC [ Cell Rep, 2023, 10.1016/j.celrep.2023.113477]	PubMed: 37979167
Targeting Lysine-Specific Demethylase 1 Rescues Major Histocompatibility Complex Class I Antigen Presentation and Overcomes Programmed Death-Ligand 1 Blockade Resistance in SCLC [ J Thorac Oncol, 2022, 17(8):1014-1031]	PubMed: 35691495
Systematic identification of biomarker-driven drug combinations to overcome resistance [ Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7]	PubMed: 35332332
Targeting histone demethylase LSD1 for treatment of deficits in autism mouse models [ Mol Psychiatry, 2022, 10.1038/s41380-022-01508-8]	PubMed: 35296809

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。