Osunprotafib
Based on 7 publication(s) in Google Scholar
Osunprotafib (ABBV-CLS-484) is an orally active and selective active site PTPN1 (IC50: 2.5 nM) and PTPN2(IC50: 1.8 nM) inhibitor. Osunprotafib has 6-8-fold weaker activity on PTPN9 and no detectable activity on SHP-1 or SHP-2. Osunprotafib increases the sensitivity of human cancer cell lines to IFNγ. Osunprotafib generates robust anti-tumor immunity by enhancing JAK-STAT signalling and reducing T cell dysfunction.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.38%
- No. CAS: 2489404-97-7
- Fòrmula: C17H24FN3O4S
- Peso molecular:385.45
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Osunprotafib
More- Nat Immunol. 2024 Oct;25(10):1943-1958. [Abstract]
- Nat Commun. 2023 Jul 27;14(1):4524. [Abstract]
- Adv Sci (Weinh). 2025 Aug;12(31):e14282. [Abstract]
- J Immunother Cancer. 2026 May 28;14(5):e014668. [Abstract]
- JCI Insight. 2024 Aug 8:e179680. [Abstract]
- Stanford University. 2025.
- Stanford University. 2025.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
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Apoptosis Analysis
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In Vivo Efficacy Study
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Flow Cytometry
Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B16 | IC50 |
0.064 μM
Compound: 7; AC-484
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Antiproliferative activity against mouse B16 cells
Antiproliferative activity against mouse B16 cells
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[PMID: 39178726] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2489404-97-7
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Appearance Solid
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Peso molecular 385.45
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Fòrmula C17H24FN3O4S
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Color White to light yellow
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SMILES
FC1=C(C[C@@H](CC2)NCCC(C)C)C2=CC(O)=C1N3CC(NS3(=O)=O)=O
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Synonyms
ABBV-CLS-484
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (7)
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Journal Impact Factor
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Most Recent
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Nat Immunol
Mapping spatial organization and genetic cell-state regulators to target immune evasion in ovarian cancer. [Abstract]2024 Oct;25(10):1943-1958. PMID: 39179931
Osunprotafib purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2024 Oct;25(10):1943-1958. [Abstract]
PTPN1/PTPN2 inhibitor (Osunprotafib; ABBV-CLS-484; 0.5, 1, 2, 4, 8, 16 μM) increased NK-mediated cytotoxicity in TYK-nu (left; 24 h) and OVCAR3 (right; 48 h) ovarian cancer cell lines in a dose-dependent manner.
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Nat Commun
2023 Jul 27;14(1):4524. PMID: 37500611 -
Adv Sci (Weinh)
PTPN2 Inhibition Disrupts Mitochondrial Renewal and Blocks TFRC-Mediated Mitophagy to Exert Anti-Tumor Activities in ALK-Positive Anaplastic Large Cell Lymphoma. [Abstract]2025 Aug;12(31):e14282. PMID: 40734623
Osunprotafib purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Aug;12(31):e14282. [Abstract]
Osunprotafib (AC484; 0-80 μM; 72 h) inhibited cell growth in SUDHL1 and Karpas299 cells in a dose-dependent manner.
Osunprotafib purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Aug;12(31):e14282. [Abstract]
Osunprotafib (AC484; 5, 10, 15 μM; 48 h) increased the expression of the cleaved forms of PARP in SUDHL1 and Karpas299 cells in a dose-dependent manner.
Osunprotafib purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Aug;12(31):e14282. [Abstract]
Osunprotafib (AC484; 5, 10, 15 μM; 48 h) induced apoptosis in Karpas299 cells and primary tumor cells, which were isolated from the hydrothorax of one ALK+ ALCL patient using annexin V-APC/7-AAD Kit.
Osunprotafib purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Aug;12(31):e14282. [Abstract]
Osunprotafib (AC484; 3 mg/kg; daily for 15 days) showed anti tumor activity in Karpas299 xenograft mouse models.
Osunprotafib purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Aug;12(31):e14282. [Abstract]
Osunprotafib (AC484; 5, 10, 15 μM; 48 h) significantly increased mitoSOX generation in Karpas299 cells.
Osunprotafib purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Aug;12(31):e14282. [Abstract]
Osunprotafib (AC484; 10 μM; 24 h) exacerbated mitochondrial damage induced by CCCP in Karpas299 cells. Mitochondrial membrane potential analysis in Karpas299 treated with 10 μm AC484 or/and 10 μm CCCP for 24 h by JC-1.
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J Immunother Cancer
CXCR3 signaling promotes Delta One T cell recruitment and antitumor efficacy in colorectal cancer. [Abstract]2026 May 28;14(5):e014668. PMID: 42208977 -
JCI Insight
2024 Aug 8:e179680. PMID: 39115957 -
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Solvente y solubilidad
DMSO : 58.33 mg/mL (151.33 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (25.94 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.5944 mL | 12.9719 mL | 25.9437 mL | 64.8593 mL |
| 5 mM | 0.5189 mL | 2.5944 mL | 5.1887 mL | 12.9719 mL | |
| 10 mM | 0.2594 mL | 1.2972 mL | 2.5944 mL | 6.4859 mL | |
| 15 mM | 0.1730 mL | 0.8648 mL | 1.7296 mL | 4.3240 mL | |
| 20 mM | 0.1297 mL | 0.6486 mL | 1.2972 mL | 3.2430 mL | |
| 25 mM | 0.1038 mL | 0.5189 mL | 1.0377 mL | 2.5944 mL | |
| 30 mM | 0.0865 mL | 0.4324 mL | 0.8648 mL | 2.1620 mL | |
| 40 mM | 0.0649 mL | 0.3243 mL | 0.6486 mL | 1.6215 mL | |
| 50 mM | 0.0519 mL | 0.2594 mL | 0.5189 mL | 1.2972 mL | |
| 60 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL | 1.0810 mL | |
| 80 mM | 0.0324 mL | 0.1621 mL | 0.3243 mL | 0.8107 mL | |
| 100 mM | 0.0259 mL | 0.1297 mL | 0.2594 mL | 0.6486 mL |
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