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MedChemExpressModel Osunprotafib -2489404-97-7

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Osunprotafib (ABBV-CLS-484) is a potent PTPN1 and PTPN2 inhibitor with subnanomolar activity. Osunprotafib has antitumor activity, enhances the immune response and increases the sensitivity of tumors to immune-mediated killing[1].
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Osunprotafib

MCE China:Osunprotafib

Brand:MedChemExpress (MCE)

Cat. No.HY-145923

CAS:2489404-97-7

Synonyms:ABBV-CLS-484

Purity:99.38%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping:Room temperature in continental US; may vary elsewhere.

Description:Osunprotafib (ABBV-CLS-484) is a potent PTPN1 and PTPN2 inhibitor with subnanomolar activity. Osunprotafib has antitumor activity, enhances the immune response and increases the sensitivity of tumors to immune-mediated killing.

In Vitro:Osunprotafib acts on both tumor cells and the host immune system, inducing unique transcriptional changes in the myeloid and lymphocyte populations of the tumor microenvironment, enhancing CD8+ T cell activation and effector functions while reducing the expression of genes classically associated with T cell depletion and dysfunction[2].

In Vivo:Osunprotafib promotes anti-tumor immunity as a monotherapy and, when combined with anti-PD-1, leads to significant tumor regression, even in models resistant to anti-PD-1 treatment, such as 4T1 and EMT6[3].

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References:

[1]. Philip R. Kym, et al. Protein tyrosine phosphatase inhibitors and methods of use thereof. WO2022056281A1.

[2]. Arvin Iracheta-Vellve, et al. Targeting the immune checkpoint PTPN2 with ABBV-CLS-484 inflames the tumor microenvironment and unleashes potent CD8+ T cell immunity. Cancer Res (2022) 82 (12_Supplement): 606.

[3]. Christina K, et al. ABBV-CLS-484: An active site PTPN2/N1 inhibitor that augments the immune response and sensitizes tumors to immune-mediated killing. Cancer Res (2022) 82 (12_Supplement): ND06.

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