製品番号: HY-145923

Osunprotafib

(別名: ABBV-CLS-484)

7 Cited Publications

カスタマーレビュー

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.

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純度: 99.38%
CAS 番号: 2489404-97-7
分子式: C₁₇H₂₄FN₃O₄S
分子量:385.45

保管条件:

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

Osunprotafib 構造式

CAS 番号: 2489404-97-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (7)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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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]

体外実験

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.

体内実験

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.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 2489404-97-7
性状 Solid
分子量 385.45
分子式 C₁₇H₂₄FN₃O₄S
Color White to light yellow
SMILES

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

ABBV-CLS-484
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

Publications (7)

All Cell Proliferation/Viability AssayWBApoptosis AnalysisIn Vivo Efficacy StudyFlow Cytometry

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Journal Impact Factor

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.
Nat Commun

A small molecule inhibitor of PTP1B and PTPN2 enhances T cell anti-tumor immunity. [Abstract]

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.
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

The HIV latency reversing agent HODHBt inhibits the phosphatases PTPN1 and PTPN2. [Abstract]

2024 Aug 8:e179680. PMID: 39115957
Stanford University

2025.
Stanford University

2025.

溶剤 & 溶解度

体外:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5944 mL

12.9719 mL

25.9437 mL

5 mM

0.5189 mL

2.5944 mL

5.1887 mL

10 mM

0.2594 mL

1.2972 mL

2.5944 mL

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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Working 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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (274 KB)
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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[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.

[4]. Baumgartner CK, et al. The PTPN2/PTPN1 inhibitor ABBV-CLS-484 unleashes potent anti-tumour immunity. Nature. 2023 Oct;622(7984):850-862. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Osunprotafib

7 Cited Publications

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Osunprotafib

MCE Bioactive Compound Library

Clinical Compound Library Plus

MedChemExpress（MCE）の使用を引用している文献 Osunprotafib

STAT アイソフォーム固有の製品をすべて表示

JAK アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (7)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Osunprotafib

MCE Bioactive Compound Library

Clinical Compound Library Plus

MedChemExpress（MCE）の使用を引用している文献 Osunprotafib

STAT アイソフォーム固有の製品をすべて表示

JAK アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (7)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Osunprotafib 関連分類

HY-145923 関連分類