Formulation: A solid
Formal Name: 5-[(7R)-1-fluoro-5,6,7,8-tetrahydro-3-hydroxy-7-[(3-methylbutyl)amino]-2-naphthalenyl]-1,2,5-thiadiazolidin-3-one, 1,1-dioxide, hydrochloride
Purity: ≥98%
Formula Markup: C17H24FN3O4S • XHCl
Formula Weight: 385,5
Shelf life (days): 1460
Notes: ABBV-CLS-484 is a dual inhibitor of protein tyrosine phosphatase 1N (PTP1N) and PTP2N (IC50s = 2.5 and 1.8 nM, respectively).{72217} It is selective for PTP1N and PTP2N over PTP6N and PTP11N (IC50s = >10 µM for both) but does inhibit PTP9N (IC50 = 15 nM). ABBV-CLS-484 (1 µM) potentiates IFN-γ-induced decreases in the proliferation of B16-F1 mouse melanoma cells. In vivo, ABBV-CLS-484 (20 mg/kg per day), in combination with an anti-PD-L1 antibody, reduces tumor volume in a B16-F1 melanoma murine model. ABBV-CLS-484 alone increases the number of CD8+ effector T cells, natural killer (NK) T cells, neutrophils, and monocytes expressing high levels of IFN-γ-induced genes, as well as increases M1 and decreases M2 macrophages, in the tumor microenvironment in the same mouse model when administered at a dose of 20 mg/kg per day.
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