1. Metabolic Enzyme/Protease Stem Cell/Wnt JAK/STAT Signaling Epigenetics Protein Tyrosine Kinase/RTK
  2. Phosphatase STAT JAK
  3. Osunprotafib

Osunprotafib  (Synonyms: ABBV-CLS-484)

Cat. No.: HY-145923 Purity: 99.38%
Handling Instructions Technical Support

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.

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CAS No. : 2489404-97-7

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
1 mg 해외재고보유
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    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.

    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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    • Biological Activity

    • 순도&문서

    • References

    • 고객리뷰

    제품 설명

    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[1][2][3][4].

    Cellular Effect
    Cell Line Type Value Description References
    B16 IC50
    0.064 μM
    Compound: 7; AC-484
    Antiproliferative activity against mouse B16 cells
    Antiproliferative activity against mouse B16 cells
    [PMID: 39178726]
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    분자량

    385.45

    화학식

    C17H24FN3O4S

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    FC1=C(C[C@@H](CC2)NCCC(C)C)C2=CC(O)=C1N3CC(NS3(=O)=O)=O

    선적

    Room temperature in continental US; may vary elsewhere.

    보관
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    용액&용해도
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5944 mL 12.9719 mL 25.9437 mL
    5 mM 0.5189 mL 2.5944 mL 5.1887 mL
    View the 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.

    • 몰농도 계산기

    • 농도 희석 계산기

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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.

    • Protocol 1

      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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (5.40 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    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.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (25.94 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    순도&문서

    Purity: 99.43%

    References

    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
    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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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    상품명:
    Osunprotafib
    Cat. No.:
    HY-145923
    수량:
    MCE Japan Authorized Agent: