Iadademstat (dihydrochloride) [1431303-72-8]

Referência HY-12782T-10mg

Tamanho : 10mg

Marca : MedChemExpress

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

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Iadademstat dihydrochloride Chemical Structure

Iadademstat dihydrochloride Chemical Structure

CAS No. : 1431303-72-8

This product is a controlled substance and not for sale in your territory.

Based on 3 publication(s) in Google Scholar

Other Forms of Iadademstat dihydrochloride:

  • Iadademstat Obtenir un devis

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Description

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

IC50 & Target

KDM1A/LSD1[1]

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.

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)CC1.07Cl.07Cl

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
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.

  • Calculateur de molarité

  • Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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
(per animal)

g

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).
Pureté et documentation
Références
  • [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.  [Content Brief]

    [2]. Tamara Maes, 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.  [Content Brief]

  • [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.

    [2]. Tamara Maes, 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.

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 3.2974 mL 16.4870 mL 32.9739 mL 82.4348 mL
H2O 5 mM 0.6595 mL 3.2974 mL 6.5948 mL 16.4870 mL
10 mM 0.3297 mL 1.6487 mL 3.2974 mL 8.2435 mL
15 mM 0.2198 mL 1.0991 mL 2.1983 mL 5.4957 mL
20 mM 0.1649 mL 0.8243 mL 1.6487 mL 4.1217 mL
25 mM 0.1319 mL 0.6595 mL 1.3190 mL 3.2974 mL
30 mM 0.1099 mL 0.5496 mL 1.0991 mL 2.7478 mL
40 mM 0.0824 mL 0.4122 mL 0.8243 mL 2.0609 mL
50 mM 0.0659 mL 0.3297 mL 0.6595 mL 1.6487 mL
60 mM 0.0550 mL 0.2748 mL 0.5496 mL 1.3739 mL
80 mM 0.0412 mL 0.2061 mL 0.4122 mL 1.0304 mL
100 mM 0.0330 mL 0.1649 mL 0.3297 mL 0.8243 mL

* 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.

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Iadademstat dihydrochloride Related Classifications

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Keywords:

Iadademstat1431303-72-8ORY-1001RG6016RO 7051790ORY1001ORY 1001RG 6016RG-6016RO7051790RO-7051790Histone DemethylaseInhibitorinhibitorinhibit

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