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Pulrodemstat

Catalog No. T39258 CAS 1821307-10-1

Synonyms: LSD1-IN-7, CC-90011

Pulrodemstat (CC-90011) is a highly potent and selective inhibitor of lysine specific demethylase-1 (LSD1). It exhibits a reversible mode of action and can be administered orally. With an impressive IC50 of 0.25 nM, Pulrodemstat effectively suppresses the enzymatic activity of LSD1. Notably, it demonstrates minimal inhibition against LSD2, MOA-A, and MAO-B enzymes. Moreover, Pulrodemstat possesses remarkable anticancer properties, promoting differentiation in acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells.

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Pulrodemstat, CAS 1821307-10-1

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5 mg	Inquiry	$ 970.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Pulrodemstat (CC-90011) is a highly potent and selective inhibitor of lysine specific demethylase-1 (LSD1). It exhibits a reversible mode of action and can be administered orally. With an impressive IC50 of 0.25 nM, Pulrodemstat effectively suppresses the enzymatic activity of LSD1. Notably, it demonstrates minimal inhibition against LSD2, MOA-A, and MAO-B enzymes. Moreover, Pulrodemstat possesses remarkable anticancer properties, promoting differentiation in acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells.
Targets&IC50	LSD1:0.25 nM (IC50)
In vitro	Pulrodemstat (CC-90011, Compound 11) efficiently induces the cellular differentiation marker CD11b in the THP-1 cell line, exhibiting an EC50 of 7 nM, and demonstrates significant antiproliferative effects in AML Kasumi-1 cells with an EC50 of 2 nM[1]. Additionally, Pulrodemstat treatment suppresses GRP in a dose-dependent manner over four days, achieving pharmacologically relevant concentrations (EC50 values of 3 nM in H209 and 4 nM in H1417 cells). Furthermore, a 12-day treatment with Pulrodemstat on SCLC cells leads to notable antiproliferative activity (EC50 of 6 nM in H1417 cells), aligning with GRP suppression[1].
In vivo	Pulrodemstat (CC-90011; 5 mg/kg; orally; daily for 30 days) effectively inhibits tumor growth in patient-derived xenograft models of small cell lung carcinoma (SCLC), showing a tumor growth inhibition rate of 78% without causing weight loss in BALB/c nude mice. Additionally, daily oral doses of Pulrodemstat for 4 days result in significant downregulation of GRP mRNA levels, achieving maximum GRP suppression at a 5 mg/kg dosage in a SCLC human tumor xenograft (H1417) mouse model. Pharmacokinetic studies reveal that, following intravenous administration, Pulrodemstat (Compound 11; 5 mg/kg) displays a systemic clearance of 32.4 mL/min/kg, an elimination half-life of 2 hours, and a high volume of distribution of 7.5 L/kg. Moreover, after oral administration, Pulrodemstat shows good absorption with an area under the curve (AUC 0-24h) of 1.8 μM·h, a maximum concentration (Cmax) of 0.36 μM, and an oral bioavailability of 32%.

Synonyms	LSD1-IN-7, CC-90011
Molecular Weight	451.478
Formula	C24H23F2N5O2
CAS No.	1821307-10-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Pulrodemstat 1821307-10-1 LSD1-IN-7 CC90011 CC-90011 CC 90011 inhibitor inhibit

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