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Pulrodemstat benzenesulfonat

Chemical Structure : Pulrodemstat benzenesulfonat

CAS No.: 2097523-60-7

Pulrodemstat benzenesulfonat (CC90011 benzenesulfonat)

Catalog No.: PC-38672Not For Human Use, Lab Use Only.

Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with biochemical IC50 of 0.3 nM.

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Biological Activity

Pulrodemstat (CC90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with biochemical IC50 of 0.3 nM.
CC-90011 inhibits gastrin-releasing peptide (GRP) mRNA expression in H209 and H1417 cell lines with IC50 of 3 nM and 4 nM, respectively.
CC-90011 exhibits potent antiproliferative activity (EC50=6 nM, H1417) that correlated with GRP suppression.
CC-90011 exhibits potent on-target induction of cellular differentiation in acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cell lines, and antitumor efficacy in patient-derived xenograft (PDX) SCLC models.

Physicochemical Properties

M.Wt 609.649
Formula C30H29F2N5O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-[2-(4-Amino-piperidin-1-yl)-5-(3-fluoro-4-methoxyphenyl)-1-methyl-6-oxo-1,6-dihydropyrimidin-4-yl]-2-fluorobenzonitrile benzenesulfonic acid

References

1. Kanouni T, et al. J Med Chem. 2020 Dec 10;63(23):14522-14529.

2. Hollebecque A, et al. Clin Cancer Res. 2021 Jan 15;27(2):438-446.

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