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 No.: 1821307-11-2
- 화학식: C24H24ClF2N5O2
- 분자량:487.93
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Pulrodemstat hydrochloride
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Biological Activity
제품 설명
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. Further protocols information, click here.
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 No. 1821307-11-2
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분자량 487.93
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
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
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pulrodemstat hydrochloride Related Classifications
HY-129388C Related Classifications
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