Iadademstat
Based on 7 publication(s) in Google Scholar
Iadademstat (ORY-1001) is a highly potent, orally active and selective LSD1 (KDM1A) inhibitor with antileukemic activity. Iadademstat can be used for relapsed or refractory acute myeloid leukemia research.
For research use only. We do not sell to patients.
- Purity : 99.82%
- CAS No.: 1431304-21-0
- Formula: C15H22N2
- Molecular Weight:230.35
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Iadademstat
More- Oncogene. 2021 Apr;40(15):2711-2724. [Abstract]
- EMBO Mol Med. 2025 Aug 29. [Abstract]
- J Med Chem. 2025 Apr 21. [Abstract]
- J Med Chem. 2024 Nov 14;67(21):19874-19888. [Abstract]
- Cell Biosci. 2022 Aug 30;12(1):140 [Abstract]
- J Appl Toxicol. 2023 Nov;43(11):1748-1760. [Abstract]
- bioRxiv. 2025 Oct 15:2025.10.13.681683. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Flow Cytometry
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In Vivo Imaging
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Flow Cytometry
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Cell Migration/Invasion Assay
Biological Activity
Description
IC50 & Target
[1]|
LSD1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Leukemia cell | EC50 |
0.1 nM
Compound: ORY-1001
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Antitumor activity against human Leukemia cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Antitumor activity against human Leukemia cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
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[PMID: 38214982] |
| MV4-11 | IC50 |
>20 μM
Compound: 2; ORY-1001
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Antiproliferative activity against human MV4-11 cells after 3 days by MTS assay
Antiproliferative activity against human MV4-11 cells after 3 days by MTS assay
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[PMID: 29031059] |
| MV4-11 | IC50 |
0.03 μM
Compound: 2; ORY-1001
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Antiproliferative activity against human MV4-11 cells after 10 days by MTS assay
Antiproliferative activity against human MV4-11 cells after 10 days by MTS assay
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[PMID: 29031059] |
| RPMI-8226 | IC50 |
>20 μM
Compound: 2; ORY-1001
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Antiproliferative activity against human RPMI8226 cells after 10 days by MTS assay
Antiproliferative activity against human RPMI8226 cells after 10 days by MTS assay
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[PMID: 29031059] |
| RPMI-8226 | IC50 |
>20 μM
Compound: 2; ORY-1001
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Antiproliferative activity against human RPMI8226 cells after 3 days by MTS assay
Antiproliferative activity against human RPMI8226 cells after 3 days by MTS assay
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[PMID: 29031059] |
| THP-1 | IC50 |
>50 μM
Compound: ORY-1001
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Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo assay
Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo assay
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[PMID: 37086699] |
In Vitro
Iadademstat (80-160 μM, 24 h-15 days) inhibits the proliferation of cancer cells H1299 and A549, arrests the cell cycle at G1 phase, induces apoptosis and inhibits the colony formation of H1299 and A549[2].
Iadademstat (80-160 μM, 24 h) decreases glycolysis in H1299 and A549 cells by reducing HK2 protein levels[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H1299 and A549
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Concentration:80-160 μM
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Incubation Time:1-4 days
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Result:Inhibited cell proliferation.
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Cell Line:H1299 and A549
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Concentration:80-160 μM
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Incubation Time:24 h
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Result:Induced apoptosis.
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Cell Line:H1299 and A549
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Concentration:80-160 μM
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Incubation Time:48 h
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Result:Arrested the cell cycle at G1 phase.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Glioblastoma xenograft mouse model[3]
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Dosage:400 µg/kg
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Administration:po, every 7 days for 28 days
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Result:Inhibited the growth of tumors, increased the survival rate.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1431304-21-0
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Appearance Solid
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Molecular Weight 230.35
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Formula C15H22N2
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Color White to off-white
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SMILES
N[C@@H]1CC[C@@](CC1)([H])N[C@H]2[C@H](C3=CC=CC=C3)C2
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Synonyms
ORY-1001
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (7)
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Journal Impact Factor
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Most Recent
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Oncogene
2021 Apr;40(15):2711-2724. PMID: 33712705 -
EMBO Mol Med
Dual targeting of CDK6 and LSD1 is synergistic and overcomes differentiation blockade in AML. [Abstract]2025 Aug 29. PMID: 40883610
Iadademstat purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2025 Aug 29. [Abstract]
MV4-11 cells cocultured with HS-5 stromal cells were incubated with CDK6 inhibitor ribociclib at 1 μM, with ORY-1001 (ORY, Iadademstat dihydrochloride) at 0.5 nM, or with the combination of ribociclib and ORY-1001 (Combo) for 96 h. After the treatment, leukemic cells were seeded in equal numbers in methylcellulose for 10 days.
Iadademstat purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2025 Aug 29. [Abstract]
MV4-11 cells transfected with control (Ctrl) or CDK6 siRNAs were incubated with 5 μM TCP or 0.5 nM ORY-1001 (ORY, Iadademstat dihydrochloride), as indicated, for 4 days. The percentage of CD11b-expressing cells was assessed by flow cytometry (left panel).
Iadademstat purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2025 Aug 29. [Abstract]
Bioluminescent imaging of NSG mice at day 24, post-xenotransplantation of 2 × 105 luciferase-labeled MOLM-14 cells. Mice were treated by intraperitoneal injections of either palbociclib (25 mg/kg), Iadademstat dihydrochloride (ORY-1001, ORY, 0.0125 mg/kg), the combination of the two molecules or vehicle control, for 4 weeks.
Iadademstat purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2025 Aug 29. [Abstract]
Quantification of hCD45 + hCD33+ leukemic blast cells in NSG mice transplanted with primary AML patient cells. Treatment with the combination of palbociclib and Iadademstat dihydrochloride (ORY-1001, ORY, 0.0125 mg/kg; i.p.) was initiated once the engraftment was confirmed by the appearance of blast cells in the bloodstream, and were administered for 3–6 weeks until an endpoint was reached. The percentage of human myeloid cells was assessed by flow cytometry in the bone marrow. PDX#1 p < 0.0001 ; PDX#2 p < 0.0001 ; PDX#3 p = 0.3301 ; PDX#4 p = 0.0033 ; PDX#5 p = 0.0368.
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J Med Chem
The Exploration of Indole-Based LSD1-Targeted Inhibitors for Enhanced Immune Response in Gastric Cancer via the PD-L1/PD-1 Axis. [Abstract]2025 Apr 21. PMID: 40257403
Iadademstat purchased from MedChemExpress. Usage Cited in: J Med Chem. 2025 Apr 21. [Abstract]
Iadademstat dihydrochloride (ORY-1001, 2 μM; 2 days) inhibited the invasion of MKN-45 cells.
Iadademstat purchased from MedChemExpress. Usage Cited in: J Med Chem. 2025 Apr 21. [Abstract]
Iadademstat dihydrochloride (ORY-1001, 2 μM) inhibited the migration of MKN-45 cells.
Iadademstat purchased from MedChemExpress. Usage Cited in: J Med Chem. 2025 Apr 21. [Abstract]
Iadademstat dihydrochloride (ORY-1001, 2 μM; 5 days) significantly reduced PD-L1 protein levels in MKN-45 and MFC cell lines.
Iadademstat purchased from MedChemExpress. Usage Cited in: J Med Chem. 2025 Apr 21. [Abstract]
Iadademstat dihydrochloride (ORY-1001, 2 μM; 5 days) reduced membrane PD-L1 levels in MKN-45 and MFC cell lines.
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J Med Chem
Target Ligand Separation and Identification of Isoforsythiaside as a Histone Lysine-Specific Demethylase 1 Covalent Inhibitor Against Breast Cancer Metastasis. [Abstract]2024 Nov 14;67(21):19874-19888. PMID: 39499621 -
Cell Biosci
Motoneurons innervation determines the distinct gene expressions in multinucleated myofibers. [Abstract]2022 Aug 30;12(1):140 PMID: 36042463 -
J Appl Toxicol
Influences of lysine-specific demethylase 1 inhibitors on NO synthase-Kruppel-like factor pathways in human endothelial cells in vitro and zebrafish (Danio rerio) larvae in vivo. [Abstract]2023 Nov;43(11):1748-1760. PMID: 37408164 -
bioRxiv
Co-targeting menin and LSD1 dismantles oncogenic programs and restores differentiation in MLL-rearranged AML. [Abstract]2025 Oct 15:2025.10.13.681683. PMID: 41279447
Solvent & Solubility
In Vitro:
DMSO : 25 mg/mL (108.53 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.85 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.85 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Olga Salamero, et al. First-in-Human Phase I Study of Iadademstat (ORY-1001): A First-in-Class Lysine-Specific Histone Demethylase 1A Inhibitor, in Relapsed or Refractory Acute Myeloid Leukemia. J Clin Oncol. 2020 Dec 20;38(36):4260-4273. [Content Brief]
[2]. Lu Z, et al., ORY-1001 Suppresses Cell Growth and Induces Apoptosis in Lung Cancer Through Triggering HK2 Mediated Warburg Effect. Front Pharmacol. 2018 Dec 4;9:1411. [Content Brief]
[3]. Yang H, et al., [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 Aug 20;44(8):1620-1630. Chinese. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.3412 mL | 21.7061 mL | 43.4122 mL | 108.5305 mL |
| 5 mM | 0.8682 mL | 4.3412 mL | 8.6824 mL | 21.7061 mL | |
| 10 mM | 0.4341 mL | 2.1706 mL | 4.3412 mL | 10.8530 mL | |
| 15 mM | 0.2894 mL | 1.4471 mL | 2.8941 mL | 7.2354 mL | |
| 20 mM | 0.2171 mL | 1.0853 mL | 2.1706 mL | 5.4265 mL | |
| 25 mM | 0.1736 mL | 0.8682 mL | 1.7365 mL | 4.3412 mL | |
| 30 mM | 0.1447 mL | 0.7235 mL | 1.4471 mL | 3.6177 mL | |
| 40 mM | 0.1085 mL | 0.5427 mL | 1.0853 mL | 2.7133 mL | |
| 50 mM | 0.0868 mL | 0.4341 mL | 0.8682 mL | 2.1706 mL | |
| 60 mM | 0.0724 mL | 0.3618 mL | 0.7235 mL | 1.8088 mL | |
| 80 mM | 0.0543 mL | 0.2713 mL | 0.5427 mL | 1.3566 mL | |
| 100 mM | 0.0434 mL | 0.2171 mL | 0.4341 mL | 1.0853 mL |
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