ORY-1001(trans)
(Synonyms: ORY-1001 dihydrochloride; RG6016 dihydrochloride; RO 7051790 dihydrochloride) 目录号 : GC36818
Iadademstat (ORY-1001) dihydrochloride 是一种选择性不可逆赖氨酸 (K) 特异性去甲基化酶 1A (KDM1A/LSD1) 抑制剂。
Cas No.:1431303-72-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
ORY-1001 trans is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor. KDM1A/LSD1[1]
ORY-1001 trans is a KDM1A inhibitor that inactivate KDM1A by irreversible binding to the flavin adenine nucleotide (FAD) cofactor. ORY-1001 trans has very high selectivity for KDM1A over the MAO enzymes, high selectivity over KDM1B and unrivaled subnanomolar cellular activity in differentiation and colony formation assays on mixed lineage leukemia (MLL)-translocated acute myeloid leukemia (AML) cell lines. ORY-1001 provokes a time and dose-dependent induction of the Cd11b differentiation marker in MLL-AF9 cells, which interestingly preceeds changes in H3K4me2 levels. While MLL-translocated cells are especially sensitive, other acute leukemia (AL) cell lines also respond to ORY-1001 trans[1].
ORY-1001 trans reduces AML tumor growth in mice and rat xenografts and increases survival time in a disseminated model of T-ALL[1].
[1]. Maes T, et al. 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.
| Cas No. | 1431303-72-8 | SDF | |
| 别名 | ORY-1001 dihydrochloride; RG6016 dihydrochloride; RO 7051790 dihydrochloride | ||
| Canonical SMILES | N[C@@H]1CC[C@@H](N[C@H]2[C@H](C3=CC=CC=C3)C2)CC1.[H]Cl.[H]Cl | ||
| 分子式 | C15H24Cl2N2 | 分子量 | 303.27 |
| 溶解度 | Water: 57.75 mg/mL (190.42 mM and warming); DMSO: 0.69 mg/mL (2.28 mM and warming) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Tranylcypromine Based Lysine-Specific Demethylase 1 Inhibitor: Summary and Perspective
J Med Chem 2020 Dec 10;63(23):14197-14215.PMID:32931269DOI:10.1021/acs.jmedchem.0c00919
Histone lysine-specific demethylase 1 (LSD1/KDM1A) has become an important and promising anticancer target since it was first identified in 2004 and specially demethylates lysine residues of histone H3K4me1/2 and H3K9me1/2. LSD1 is ubiquitously overexpressed in diverse cancers, and abrogation of LSD1 results in inhibition of proliferation, invasion, and migration in cancer cells. Over the past decade, a number of biologically active small-molecule LSD1 inhibitors have been developed. To date, six trans-2-phenylcyclopropylamine (TCP)-based LSD1 inhibitors (including TCP, ORY-1001, GSK-2879552, INCB059872, IMG-7289, and ORY-2001) that covalently bind to the flavin adenine dinucleotide (FAD) within the LSD1 catalytic cavity have already entered into clinical trials. Here, we provide an overview about the structures, activities, and structure-activity relationship (SAR) of TCP-based LSD1 inhibitors that mainly covers the literature from 2008 to date. The opportunities, challenges, and future research directions in this emerging and promising field are also discussed.