Art. -Nr.: HY-129388A

Pulrodemstat

(Synonyms: CC-90011; LSD1-IN-7)

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC₅₀ of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MAO-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.

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Reinheit: 98.86%
CAS. Nr.: 1821307-10-1
Formel: C₂₄H₂₃F₂N₅O₂
Molecular Weight:451.47

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Pulrodemstat Chemical Structure

CAS. Nr.: 1821307-10-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

KDM1/LSD1

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen :

In Vitro

Pulrodemstat (CC-90011, Compound 11) shows potent induction of on-target cellular differentiation marker CD11b in THP-1 cell line with an EC₅₀ of 7 nM, antiproliferative activity in AML kasumi-1 cells with an EC₅₀ of 2 nM^[1].
Suppression of GRP is observed with treatment of Pulrodemstat (4 days) in a dose-dependent manner and at pharmacologically useful concentrations (EC₅₀=3 nM, H209 and 4 nM, H1417). Pulrodemstat (12 days) treatment of SCLC cells results in potent antiproliferative activity (EC₅₀=6 nM, H1417) that correlated with GRP suppression^[1].

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

In Vivo

Pulrodemstat (CC-90011; 5 mg/kg; oral administration; daily; for 30 days; for 30 days) treatment inhibits tumor growth in patient-derived xenograft SCLC models^[1].
Pulrodemstat (once a day; for 4 days) treatment results in robust downregulation of GRP mRNA levels at 2.5 mg/kg and maximum suppression of GRP at 5 mg/kg in a SCLC human tumor xenograft (H1417) mice^[1].
After i.v. administration, Pulrodemstat (Compound 11; 5 mg/kg) has systemic clearance of 32.4 mL/min/kg, elimination half-life of 2 h, and a high volume of distribution of 7.5 L/kg. Pulrodemstat (Compound 11; 5 mg/kg) is readily absorbed after oral administration with an AUC_0-24h of 1.8 μM·h, C_max of 0.36 μM, and oral bioavailability of 32%^[1].

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

Animal Model:

BALB/c nude mice bearing small cell lung carcinoma (SCLC)^[1]
Dosage:

5 mg/kg
Administration:

Oral administration; daily; for 30 days
Result:

Showed a tumor growth inhibition (TGI) of 78% at 5 mg/kg with no body weight loss.

Chemical Information

CAS. Nr. 1821307-10-1
Appearance Solid
Molecular Weight 451.47
Formel C₂₄H₂₃F₂N₅O₂
Color White to off-white
SMILES

N#CC1=CC=C(C(N=C(N2CCC(N)CC2)N3C)=C(C4=CC=C(OC)C(F)=C4)C3=O)C=C1F
Synonyms

CC-90011; LSD1-IN-7
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (4)

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Journal Impact Factor

Proc Natl Acad Sci U S A

Discovery of an LSD1 PROTAC degrader. [Abstract]

2025 May 20;122(20):e2425812122. PMID: 40366693
Eur J Med Chem

Novel acridine-based LSD1 inhibitors enhance immune response in gastric cancer. [Abstract]

2023 Nov 5:259:115684. PMID: 37542989
Clin Exp Med

Corin: a dual inhibitor for KDM1A/HDAC1, suppresses hepatocellular carcinoma by triggering cuproptosis. [Abstract]

2025 Nov 25;26(1):33. PMID: 41286164
ACS Pharmacol Transl Sci

Comprehensive in Vitro Characterization of the LSD1 Small Molecule Inhibitor Class in Oncology. [Abstract]

2021 Nov 12;4(6):1818-1834. PMID: 34927013

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (110.75 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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2150 mL

11.0749 mL

22.1499 mL

5 mM

0.4430 mL

2.2150 mL

4.4300 mL

10 mM

0.2215 mL

1.1075 mL

2.2150 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.54 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Toufike Kanouni, et al. Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1). J Med Chem. 2020 Dec 10;63(23):14522-14529. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.2150 mL	11.0749 mL	22.1499 mL	55.3747 mL
	5 mM	0.4430 mL	2.2150 mL	4.4300 mL	11.0749 mL
	10 mM	0.2215 mL	1.1075 mL	2.2150 mL	5.5375 mL
	15 mM	0.1477 mL	0.7383 mL	1.4767 mL	3.6916 mL
	20 mM	0.1107 mL	0.5537 mL	1.1075 mL	2.7687 mL
	25 mM	0.0886 mL	0.4430 mL	0.8860 mL	2.2150 mL
	30 mM	0.0738 mL	0.3692 mL	0.7383 mL	1.8458 mL
	40 mM	0.0554 mL	0.2769 mL	0.5537 mL	1.3844 mL
	50 mM	0.0443 mL	0.2215 mL	0.4430 mL	1.1075 mL
	60 mM	0.0369 mL	0.1846 mL	0.3692 mL	0.9229 mL
	80 mM	0.0277 mL	0.1384 mL	0.2769 mL	0.6922 mL
	100 mM	0.0221 mL	0.1107 mL	0.2215 mL	0.5537 mL

Keywords

Pulrodemstat

4 Cited Publications

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Pulrodemstat

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) Pulrodemstat

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Pulrodemstat

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) Pulrodemstat

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Pulrodemstat Related Classifications

HY-129388A Related Classifications