Pulrodemstat hydrochloride
Based on 4 publication(s) in Google Scholar
Pulrodemstat (CC-90011) hydrochloride is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 value of 0.25 nM. Pulrodemstat hydrochloride is less enzymatic inhibition against LSD2, MAO-A, and MAO-B. Pulrodemstat hydrochloride induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
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- CAS. Nr.: 1821307-11-2
- Formel: C24H24ClF2N5O2
- Molecular Weight:487.93
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
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KDM1/LSD1 |
In Vitro
Pulrodemstat (Compound 11) hydrochloride 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) hydrochloride in a dose-dependent manner and at pharmacologically useful concentrations (EC50=3 nM, H209 and 4 nM, H1417). Pulrodemstat (12 days) hydrochloride 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 (once a day; for 4 days) hydrochloride 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) hydrochloride 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) hydrochloride is readily absorbed after oral administration with an AUC0-24h of 1.8 μM·h, Cmax 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.
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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. Nr. 1821307-11-2
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Molecular Weight 487.93
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Formel C24H24ClF2N5O2
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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.Cl
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Synonyms
CC-90011 hydrochloride; LSD1-IN-7 hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
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
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Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Pulrodemstat hydrochloride Related Classifications
HY-129388C Related Classifications
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