ABBV-CLS-484 | Dual PTPN2/N1 inhibitor

Chemical Structure : ABBV-CLS-484

CAS No.: 2489404-97-7

ABBV-CLS-484 (Osunprotafib, AC484, AC 484)

Catalog No.: PC-73317Not For Human Use, Lab Use Only.

ABBV-CLS-484 (AC484) is a first-in-class, orally bioavailable, potent and selective PTPN2 and PTPN1 active-site inhibitor with IC50 of 1.8 and 2.5 nM, respectively.

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Biological Activity

ABBV-CLS-484 (AC484, Osunprotafib) is a first-in-class, orally bioavailable, potent and selective PTPN2 and PTPN1 active-site inhibitor with IC50 of 1.8 and 2.5 nM, respectively.

ABBV-CLS-484 (AC484) demonstrates high selectivity for PTPN2/N1, with 6-8-fold weaker activity on PTPN9 and no detectable activity on SHP-1 or SHP-2.

ABBV-CLS-484 (AC484) shows no off-target activity for a diverse panel of phosphatases, kinases and other receptors, including the hERG channel.

ABBV-CLS-484 (AC484) increases IFNγ-mediated STAT1 phosphorylation in B16 tumour cells with EC50 of 176 nM.

ABBV-CLS-484 (AC484) phenocopies the effects of deletion of both Ptpn2 and Ptpn1 on cell growth and ISG expression in response to IFN, and enhances tumour sensitivity to T cell-mediated toxicity in tumor cells.

ABBV-CLS-484 (AC484) enhances T cell function in vitro, which is more potently than single targeting approaches.

ABBV-CLS-484 (AC484) induces immune-dependent tumour regression in various syngeneic and metastatic mouse models, shows efficacy in a broader range of contexts alone or in combination with anti-PD-1.

ABBV-CLS-484 (AC484) inflames the tumour microenvironment and promotes natural killer cell and CD8+ T cell function by enhancing JAK–STAT signalling and reducing T cell dysfunction.

Physicochemical Properties

M.Wt	385.454
Formula	C17H24FN3O4S
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	(R)-5-(1-fluoro-3-hydroxy-7-(isopentylamino)-5,6,7,8-tetrahydronaphthalen-2-yl)-1,2,5-thiadiazolidin-3-one 1,1-dioxide

References

1. Baumgartner CK, et al. Nature. 2023 Oct 4. doi: 10.1038/s41586-023-06575-7.

2. Liang S, et al. Nat Commun. 2023 Jul 27;14(1):4524.

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ABBV-CLS-484 (Osunprotafib, AC484, AC 484)

Biological Activity

Physicochemical Properties

References

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