| Name | Pulrodemstat |
| 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. |
| In vitro | Pulrodemstat (CC-90011, Compound 11) shows potent induction of on-target cellular differentiation marker CD11b in THP-1 cell line with an EC 50 of 7 nM, antiproliferative activity in AML kasumi-1 cells with an EC 50 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 (EC 50 =3 nM, H209 and 4 nM, H1417). Pulrodemstat (12 days) treatment of SCLC cells results in potent antiproliferative activity (EC 50 =6 nM, H1417) that correlated with GRP suppression[1]. |
| 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/sub>max of 0.36 μM, and oral bioavailability of 32%[1]. 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Keywords | CC90011 | Pulrodemstat | CC 90011 |
