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Reagentes e instrumentos para imunologia, biologia celular e biologia molecular.

Iadademstat (dihydrochloride) [1431303-72-8]

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Referência HY-12782T-10mg

Tamanho : 10mg

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Marca : MedChemExpress

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Contactar o distribuidor local :

Telefone : +1 850 650 7790

Description

Iadademstat (ORY-1001) dihydrochloride is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.

IC₅₀ & Target

KDM1/LSD1

Cellular Effect

Cell Line	Type	Value	Description	References
AGS	IC₅₀	> 50 μM Compound: ORY-1001	Antiproliferative activity against human AGS cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human AGS cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 33957387]
BGC-823	IC₅₀	> 50 μM Compound: ORY-1001	Antiproliferative activity against human BGC-823 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human BGC-823 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 33957387]
MKN-1	IC₅₀	> 50 μM Compound: ORY-1001	Antiproliferative activity against human MKN-1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MKN-1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 33957387]
MKN-45	IC₅₀	> 50 μM Compound: ORY-1001	Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 33957387]
NCI-N87	IC₅₀	> 50 μM Compound: ORY-1001	Antiproliferative activity against human NCI-N87 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-N87 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 33957387]
SNU1	IC₅₀	> 50 μM Compound: ORY-1001	Antiproliferative activity against human SNU1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SNU1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 33957387]
THP-1	IC₅₀	> 20 μM Compound: ORY-1001	Antiproliferative activity against human THP1 cells after 8 days by MTS assay Antiproliferative activity against human THP1 cells after 8 days by MTS assay	[PMID: 30448189]

In Vitro

Iadademstat dihydrochloride is a KDM1A inhibitor that inactivate KDM1A by irreversible binding to the flavin adenine nucleotide (FAD) cofactor. Iadademstat 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. Iadademstat 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 Iadademstat^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Iadademstat reduces AML tumor growth in mice and rat xenografts and increases survival time in a disseminated model of T-ALL^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

Masse moléculaire

303.27

Formule

C₁₅H₂₄Cl₂N₂

CAS No.

1431303-72-8

Appearance

Solid

Color

White to off-white

SMILES

N[C@@H]1CC[C@@H](N[C@H]2[C@H](C3=CC=CC=C3)C2)CC1.20Cl.20Cl

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvant et solubilité

In Vitro:

H₂O : 57.75 mg/mL (190.42 mM; Need ultrasonic and warming)

DMSO : 0.69 mg/mL (2.28 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.2974 mL	16.4870 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

View the 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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.

Protocol 1

Add each solvent one by one: PBS
Solubility: 100 mg/mL (329.74 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
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Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).