Osunprotafib

SKU: orb1688337

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Description

Osunprotafib (ABBV-CLS-484) is a potent, orally bioavailable inhibitor of PTP1B and PTPN2 currently in clinical trials for the treatment of solid tumors. It modulates the tumor microenvironment by boosting natural killer cell and CD8 T cell activity, enhancing anti-tumor immunity through activation of JAK–STAT signaling, and mitigating T cell dysfunction.

Research Area

Metabolism Research

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Key Properties

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CAS Number	2489404-97-7
MW	385.45
Purity	99.91%
Formula	C₁₇H₂₄FN₃O₄S
SMILES	CC(C)CCN[C@@H]1CCc2cc(O)c(N3CC(=O)NS3(=O)=O)c(F)c2C1
Target	Phosphatase
Solubility	DMSO: 56.2 mg/mL (145.9 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble)

Bioactivity

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Target IC50	PTP2N:1.8 nM\|PTPN2/PTPN1:0.176 μM (EC50)\|PTP1N:2.5 nM
In Vivo	METHODS: Mice with systemic Ptpn2 deletion were administered oral doses of Osunprotafib (ABBV-CLS-484) at 3/10/100 mg/kg twice daily in an attempt to determine whether oral systemic Inhibition of PTPN2/N1 could be a safe and effective immunotherapy RESULTS Circulating chemokines, including CXCL10 and CXCL9, increased 2-3-fold at a dose of 10 mg kg-1 twice daily; a dose of 100 mg/kg twice daily resulted in significant Systemic immune activation, manifested by significant increases in circulating cytotoxic granzyme B (GZMB) CD8 T cells and cytokines such as CXCL10 and CXCL9. METHODS: Animals with tumors were evaluated at doses of 50, 100, and 150 mg/kg-1 once daily and significant Changes in body condition score or body weight were observed. Results No significant Changes in body weight were observed with Osunprotafib (ABBV-CLS-484), which was tolerated in naive rats at doses up to 300 mg kg-1/day for 28 days the most notable finding was a dose-dependent infiltration of immune cells in the kidneys, joints and liver, and it was also found that Osunprotafib (ABBV-CLS-484) has a relatively short half-life, allowing for rapid discontinuation of treatment, and thus faster than antibody-based therapies. effectively resolve inflammatory conditions. Read more...
In Vitro	Osunprotafib (ABBV-CLS-484) dose-dependently increased STAT5 phosphorylation to similar levels in whole blood from healthy donors and cancer patients; Osunprotafib (ABBV-CLS-484) increased IFNγ-induced STAT1 phosphorylation and CXCL10 production in blood Samples from healthy donors and cancer patients, suggesting that Osunprotafib (ABBV-CLS-484)-enhanced pathway engagement leads to enhanced downstream functional effects; Osunprotafib (ABBV-CLS-484) increased T cell activation and function in human whole blood, as indicated by dose-dependent increases in CD69 expression and IFNγ and TNF production after TCR stimulation; Osunprotafib (ABBV-CLS-484) Inhibition of PTPN2/N1 enhances human immune cell activation. Read more...

Storage & Handling

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Storage	Powder: -20°C
Disclaimer	For research use only

Alternative Names

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Osunprotafib, AC 484, AC 484, ABBV-CLS 484, ABBV-CLS484, ABBV-CLS-484, AC484, AC-484, protein tyrosine phosphatase(PTP)

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Cas No. 2489404-97-7

Compound Identifiers

PubChem CID

155103607 ↗

Key Properties

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No computed properties available.

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Purity:	>98%
CAS Number:	2489404-97-7
MW:	385.45
Formula:	C₁₇H₂₄FN₃O₄S

Osunprotafib

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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ABBV-CLS-484 [orb1818874]

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