Pulrodemstat benzenesulfonate
Based on 4 publication(s) in Google Scholar
Pulrodemstat (CC-90011) benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat benzenesulfonate is less enzymatic inhibition against LSD2, MAO-A, and MAO-B. Pulrodemstat benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
For research use only. We do not sell to patients.
- Purity: 99.64%
- CAS No.: 2097523-60-7
- Formula: C30H29F2N5O5S
- Molecular Weight:609.64
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Pulrodemstat benzenesulfonate
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Biological Activity
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KDM1/LSD1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| IMR-90 | EC50 |
>10 μM
Compound: 11; CC-90011
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Anti-proliferative activity in human IMR-90 cells incubated for 168 hrs by MTS assay
Anti-proliferative activity in human IMR-90 cells incubated for 168 hrs by MTS assay
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[PMID: 33034194] |
| Kasumi 1 | EC50 |
2 nM
Compound: 11; CC-90011
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Anti-proliferative activity in human Kasumi 1 cells incubated for 168 hrs by MTS assay
Anti-proliferative activity in human Kasumi 1 cells incubated for 168 hrs by MTS assay
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[PMID: 33034194] |
| Kasumi 1 | IC50 |
2 nM
Compound: CC-90011
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Antiproliferative activity against human Kasumi 1 cells assessed as inhibition of cell proliferation and measured after 7 days by CellTiter-Glo assay
Antiproliferative activity against human Kasumi 1 cells assessed as inhibition of cell proliferation and measured after 7 days by CellTiter-Glo assay
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[PMID: 38214982] |
| MV4-11 | IC50 |
1.4 μM
Compound: CC-90011
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Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
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[PMID: 38214982] |
| THP-1 | IC50 |
7 nM
Compound: CC-90011
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Cytotoxicity against human THP-1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Cytotoxicity against human THP-1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
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[PMID: 38214982] |
Pulrodemstat (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.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice bearing small cell lung carcinoma (SCLC)[1]
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Dosage:5 mg/kg
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Administration:Oral administration; daily; for 30 days
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Result:Showed a tumor growth inhibition (TGI) of 78% at 5 mg/kg with no body weight loss.
Chemical Information
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CAS No. 2097523-60-7
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Appearance Solid
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Molecular Weight 609.64
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Formula C30H29F2N5O5S
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Color Off-white to light yellow
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SMILES
N#CC1=CC=C(C(N=C(N2CCC(N)CC2)N3C)=C(C4=CC=C(OC)C(F)=C4)C3=O)C=C1F.O=S(C5=CC=CC=C5)(O)=O
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Synonyms
CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (4)
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Journal Impact Factor
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Most Recent
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Proc Natl Acad Sci U S A
2025 May 20;122(20):e2425812122. PMID: 40366693 -
Eur J Med Chem
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
Solvent & Solubility
DMSO : 50 mg/mL (82.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
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 | 1 mM | 1.6403 mL | 8.2016 mL | 16.4031 mL | 41.0078 mL |
| 5 mM | 0.3281 mL | 1.6403 mL | 3.2806 mL | 8.2016 mL | |
| 10 mM | 0.1640 mL | 0.8202 mL | 1.6403 mL | 4.1008 mL | |
| 15 mM | 0.1094 mL | 0.5468 mL | 1.0935 mL | 2.7339 mL | |
| 20 mM | 0.0820 mL | 0.4101 mL | 0.8202 mL | 2.0504 mL | |
| 25 mM | 0.0656 mL | 0.3281 mL | 0.6561 mL | 1.6403 mL | |
| 30 mM | 0.0547 mL | 0.2734 mL | 0.5468 mL | 1.3669 mL | |
| 40 mM | 0.0410 mL | 0.2050 mL | 0.4101 mL | 1.0252 mL | |
| 50 mM | 0.0328 mL | 0.1640 mL | 0.3281 mL | 0.8202 mL | |
| 60 mM | 0.0273 mL | 0.1367 mL | 0.2734 mL | 0.6835 mL | |
| 80 mM | 0.0205 mL | 0.1025 mL | 0.2050 mL | 0.5126 mL |
Pulrodemstat benzenesulfonate Related Classifications
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