Iadademstat dihydrochloride (Synonyms: ORY-1001 dihydrochloride; RG6016 dihydrochloride; RO 7051790 dihydrochloride)

Name: Iadademstat dihydrochloride
Brand: MedChemExpress
SKU: HY-12782T
Rating: 5.0 (7 reviews)

Cat. No.: HY-12782T Purity: 99.98%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Iadademstat dihydrochloride 화학구조

CAS No. : 1431303-72-8

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

or 대량구매 문의

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

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

고객리뷰

Based on 7 publication(s) in Google Scholar

Other Forms of Iadademstat dihydrochloride:

Iadademstat In-stock

7 Publications Citing Use of MCE Iadademstat dihydrochloride

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Demethylase Isoform Specific Products:

View All Isoforms

KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

Biological Activity
순도&문서
References
고객리뷰

제품 설명

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 3 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]
MM1.S	EC₅₀	> 10 3 Compound: ORY-1001	Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability after 144 hrs Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability after 144 hrs	[PMID: 33359604]
BGC-823	IC₅₀	>50 3 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 3 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 3 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]
AGS	IC₅₀	> 50 3 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 3 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]
NCI-N87	IC₅₀	>50 3 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]
MKN-1	IC₅₀	> 50 3 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]
SNU1	IC₅₀	>50 3 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 3 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]
MKN-45	IC₅₀	> 50 3 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 3 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 3 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 3 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.

분자량

303.27

화학식

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.[H]Cl.[H]Cl

선적

Room temperature in continental US; may vary elsewhere.

보관

4°C, sealed storage, away from moisture

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

용액&용해도

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.

몰농도 계산기
농도 희석 계산기

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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)

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).

순도&문서

Purity: 99.98%

Select Batch:

Data Sheet (273 KB) SDS (393 KB)

COA (247 KB) HNMR (277 KB) LCMS (88 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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.

Iadademstat dihydrochloride Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

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

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Iadademstat dihydrochloride (Synonyms: ORY-1001 dihydrochloride; RG6016 dihydrochloride; RO 7051790 dihydrochloride)

고객리뷰

Other Forms of Iadademstat dihydrochloride:

Iadademstat dihydrochloride Related Antibodies

7 Publications Citing Use of MCE Iadademstat dihydrochloride

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Demethylase Isoform Specific Products:

Biological Activity

순도&문서

References

고객리뷰

Iadademstat dihydrochloride Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Iadademstat dihydrochloride Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report