Iadademstat (Synonyms: ORY-1001)

Name: Iadademstat
Brand: MedChemExpress
SKU: HY-109117
Rating: 5.0 (7 reviews)

Cat. No.: HY-109117 Purity: 99.82%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

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Iadademstat 화학구조

CAS No. : 1431304-21-0

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	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	견적 받기
200 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:

Iadademstat dihydrochloride In-stock

7 Publications Citing Use of MCE Iadademstat

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

IC₅₀ & Target^[1]

LSD1

Cellular Effect

Cell Line	Type	Value	Description	References
Leukemia cell	EC₅₀	0.1 nM Compound: ORY-1001	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	[PMID: 38214982]
THP-1	IC₅₀	> 50 μM Compound: ORY-1001	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	[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.

Cell Proliferation Assay^[2]

Cell Line:	H1299 and A549
Concentration:	80-160 μM
Incubation Time:	1-4 days
Result:	Inhibited cell proliferation.

Apoptosis Analysis^[2]

Cell Line:	H1299 and A549
Concentration:	80-160 μM
Incubation Time:	24 h
Result:	Induced apoptosis.

Cell Cycle Analysis^[2]

Cell Line:	H1299 and A549
Concentration:	80-160 μM
Incubation Time:	48 h
Result:	Arrested the cell cycle at G1 phase.

In Vivo

Iadademstat (400 µg/kg, po, every 7 days for 28 days) exhibits antitumor activity in glioblastoma xenograft mouse model^[3].

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

Animal Model:	Glioblastoma xenograft mouse model^[3]
Dosage:	400 µg/kg
Administration:	po, every 7 days for 28 days
Result:	Inhibited the growth of tumors, increased the survival rate.

Clinical Trial

분자량

230.35

화학식

C₁₅H₂₂N₂

CAS No.

1431304-21-0

Appearance

Solid

Color

White to off-white

SMILES

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

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

용액&용해도

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.3412 mL	21.7061 mL	43.4122 mL
5 mM	0.8682 mL	4.3412 mL	8.6824 mL
10 mM	0.4341 mL	2.1706 mL	4.3412 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, 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.

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:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (10.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

순도&문서

Purity: 99.82%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (245 KB) HNMR (139 KB) RP-HPLC (168 KB) LCMS (106 KB)

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

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

Iadademstat 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:

Iadademstat1431304-21-0ORY-1001ORY1001ORY 1001Histone DemethylaseApoptosisKDM1ALSD1antileukemic activityrefractory acute myeloid leukemiaInhibitorinhibitorinhibit

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Iadademstat (Synonyms: ORY-1001)

고객리뷰

Other Forms of Iadademstat:

Iadademstat Related Antibodies

7 Publications Citing Use of MCE Iadademstat

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Demethylase Isoform Specific Products:

Biological Activity

순도&문서

References

고객리뷰

Iadademstat Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Iadademstat Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report