Drug intelligence / Profile preview

SBI-183

Development stage
Preclinical
Lead developer
Sapphire Biotech
Modality
Small Molecules
Administration
Oral
01

Overview

SBI-183 is an orally active small molecule inhibitor of Quiescin sulfhydryl oxidase 1 (QSOX1), with a dissociation constant (Kd) of 20 μM. QSOX1 is an enzyme overexpressed in various tumor types and catalyzes the formation of disulfide bonds in proteins. Inhibition of QSOX1 by SBI-183 suppresses the proliferative and invasive phenotypes of several cancer cell lines, including renal carcinoma (786-O, RCJ-41T2), triple-negative breast cancer (MDA-MB-231), lung adenocarcinoma (A549), and pancreatic ductal adenocarcinoma (MIA PaCa2). In vivo studies have shown that oral administration of SBI-183 inhibits tumor growth in human xenograft mouse models of renal cell carcinoma. The compound does not affect the viability of nonmalignant cells such as fibroblasts or rapidly proliferating PBMCs at effective concentrations[1][2][3][4][5][7]. It is being developed by Sanford Burnham Prebys Medical Discovery Institute.

Other names
3-methoxy-N-[4-(1-pyrrolidinyl)phenyl]benzamideCAS 625403-59-0CAS625403-59-0CAS-625403-59-0
02

Targets

QSOX1 (Quiescin sulfhydryl oxidase 1)

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