2. Epigenetics Apoptosis
  3. Histone Demethylase Apoptosis
  4. Iadademstat

Iadademstat  (Synonyms: ORY-1001)

製品番号: HY-109117 純度: 99.82%
COA 取扱説明書 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

Iadademstat 構造式

CAS 番号 : 1431304-21-0

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 121 在庫あり
Solution
10 mM * 1 mL in DMSO USD 121 在庫あり
Solid
5 mg $110 在庫あり
10 mg $180 在庫あり
25 mg $370 在庫あり
50 mg $700 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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

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Based on 7 publication(s) in Google Scholar

Other Forms of Iadademstat:

Iadademstat 関連抗体

Top Publications Citing Use of Products

Histone Demethylase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

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[1].

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]
MV4-11 IC50
>20 μM
Compound: 2; ORY-1001
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
[PMID: 29031059]
MV4-11 IC50
0.03 μM
Compound: 2; ORY-1001
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
[PMID: 29031059]
RPMI-8226 IC50
>20 μM
Compound: 2; ORY-1001
Antiproliferative activity against human RPMI8226 cells after 10 days by MTS assay
Antiproliferative activity against human RPMI8226 cells after 10 days by MTS assay
[PMID: 29031059]
RPMI-8226 IC50
>20 μM
Compound: 2; ORY-1001
Antiproliferative activity against human RPMI8226 cells after 3 days by MTS assay
Antiproliferative activity against human RPMI8226 cells after 3 days by MTS assay
[PMID: 29031059]
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]
体外実験

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.

Iadademstat 関連抗体

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.
体内実験

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.
臨床実験
分子量

230.35

分子式

C15H22N2
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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.
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.
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.
純度とドキュメンテーション
参考文献

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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Iadademstat Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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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製品番号:
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