Pulrodemstat benzenesulfonate  (Synonyms: CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate)

CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC₅₀ of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity^[1].

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 CC-90011 (4 days) in a dose-dependent manner and at pharmacologically useful concentrations (EC₅₀=3 nM, H209 and 4 nM, H1417). CC-90011 (12 days) treatment of SCLC cells results in potent antiproliferative activity (EC₅₀=6 nM, H1417) that correlated with GRP suppression^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CC-90011 (5 mg/kg; oral administration; daily; for 30 days) treatment inhibits tumor growth in patient-derived xenograft SCLC models^[1].
CC-90011 (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, CC-90011 (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. CC-90011 (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

609.64

Solid

C₃₀H₂₉F₂N₅O₅S

2097523-60-7

N#CC1=CC=C(C(N=C(N2CCC(N)CC2)N3C)=C(C4=CC=C(OC)C(F)=C4)C3=O)C=C1F.O=S(C5=CC=CC=C5)(O)=O

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

• [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.  [Content Brief]