1821307-10-1
1821307-10-1 structure
- Name: Pulrodemstat
- Chemical Name: Pulrodemstat
- CAS Number: 1821307-10-1
- Molecular Formula: C24H23F2N5O2
- Molecular Weight: 451.47
- Catalog: Signaling Pathways Epigenetics Histone Demethylase
- Create Date: 2021-12-25 23:53:14
- Modify Date: 2024-01-07 17:56:13
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Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity[1].
| Name | Pulrodemstat |
|---|
| Description | Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity[1]. |
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| Related Catalog | |
| Target |
IC50: 0.25 nM (LSD1)[1] |
| In Vitro | Pulrodemstat (CC-90011, 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]. |
| 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 AUC0-24h 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. |
| References |
| Molecular Formula | C24H23F2N5O2 |
|---|---|
| Molecular Weight | 451.47 |