Referencia número: HY-107429

Abrocitinib

(Synonyms: PF-04965842)

11 Cited Publications

Revisión del cliente

Based on 11 publication(s) in Google Scholar

Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC₅₀s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC₅₀, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease.

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Pureza: 99.26%
No. CAS: 1622902-68-4
Fòrmula: C₁₄H₂₁N₅O₂S
Peso molecular:323.41

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Abrocitinib Chemical Structure

No. CAS: 1622902-68-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (11)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

JAK1

29 nM (IC₅₀)

JAK2

803 nM (IC₅₀)

Tyk2

1253 nM (IC₅₀)

Ver todos los productos específicos de isoformas JAK :

Cellular Effect

Cell Line	Type	Value	Description	References
TF-1	IC₅₀	1.4 μM Compound: Abrocitinib	Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay	[PMID: 32462873]

In Vitro

Abrocitinib (Compound 25) inhibits IFNα-stimulated phosphorylation of STAT3, IFN-stimulated phosphorylation of STAT1 in human whole blood (HWB), as well as pSTAT5 in CD34+ spiked into HWB (JAK2), with IC₅₀s of 189, 163 nM, 7.178 μM, respectively^[1].

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

In Vivo

Abrocitinib (Compound 25; 5, 15, 50 mg/kg, p.o., daily for 7 days) significantly reduces paw swelling in rat adjuvant-induced arthritis model^[1].

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

Animal Model:

Female Lewis rats (8−10 weeks old)^[1]
Dosage:

5, 15, 50 mg/kg
Administration:

P.O. daily for 7 days
Result:

Obviously reduced paw swelling at all doses.

Ensayo clínico

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

Chemical Information

No. CAS 1622902-68-4
Appearance Solid
Peso molecular 323.41
Fòrmula C₁₄H₂₁N₅O₂S
Color White to light yellow
SMILES

CN([C@H]1C[C@@H](NS(CCC)(=O)=O)C1)C2=C3C(NC=C3)=NC=N2
Synonyms

PF-04965842
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (11)

All Cell Proliferation/Viability AssayCell Imaging/StainingWBFlow Cytometry

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Journal Impact Factor

Cancer Res

JAK-STAT Signaling in Inflammatory Breast Cancer Enables Chemotherapy-Resistant Cell States. [Abstract]

2023 Jan 18;83(2):264-284. PMID: 36409824
Nat Commun

CDK2 inhibitor BLU-222 synergizes with CDK4/6 inhibitors in drug resistant breast cancers through p21/p27 induction. [Abstract]

2026 Jan 22;17(1):619. PMID: 41571637

Abrocitinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2026 Jan 22;17(1):619. [Abstract]

Cell viability assays in MCF7 Par and PR, T47D Par and PR, and MDA-MB-231 Par and PR cells treated with Abrocitinib (ABR) (1 μM; 5 d).
J Immunother Cancer

Combinatorial treatment with upadacitinib abrogates systemic toxicity of a tumor-targeted IL-2 fusion protein. [Abstract]

2025 May 11;13(5):e010831. PMID: 40350206
Mol Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929
Int J Mol Sci

JAK Signaling Is Critically Important in Cytokine-Induced Viral Susceptibility of Keratinocytes. [Abstract]

2023 May 25;24(11):9243. PMID: 37298195

Abrocitinib purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2023 May 25;24(11):9243. [Abstract]

Abrocitinib (50-200 nM; 24 h) significantly decreased VV (poxvirus) plaque number in IL-4 + IL-13-treated KC cultures.
Int J Mol Sci

Antifibrotic TSG-6 Expression Is Synergistically Increased in Both Cells during Coculture of Mesenchymal Stem Cells and Macrophages via the JAK/STAT Signaling Pathway. [Abstract]

2022 Oct 28;23(21):13122. PMID: 36361907
Bioorg Chem

Baicalin ameliorates 2,4-dinitrochlorobenzene-induced atopic dermatitis-like skin lesions in mice through modulating skin barrier function, gut microbiota and JAK/STAT pathway. [Abstract]

2022 Feb:119:105538. PMID: 34929516

Abrocitinib purchased from MedChemExpress. Usage Cited in: Bioorg Chem. 2022 Feb:119:105538. [Abstract]

Abrocitinib (AB) (7.5 mg/kg; i.g.; once daily for 14 d) reduced the protein expression of TSLP and IVL, while up-regulated the protein expressions of FLG and LOR in dorsal skin of the DNCB-treated mice.

Abrocitinib purchased from MedChemExpress. Usage Cited in: Bioorg Chem. 2022 Feb:119:105538. [Abstract]

Abrocitinib (AB) (7.5 mg/kg; i.g.; once daily for 14 d) significantly decreased the ratio of p-IκBα/IκBα and p-p65/p65, and increased the expression level of IκBα in the nucleus in the dorsal skin of the DNCB-treated mice.
Clin Immunol

Development and validation of a flow cytometry-based ISG15 induction assay to monitor the type I interferon response. [Abstract]

2026 Feb:283:110654. PMID: 41344526

Abrocitinib purchased from MedChemExpress. Usage Cited in: Clin Immunol. 2026 Feb:283:110654. [Abstract]

The JAK1 inhibitor Abrocitinib (300 μM) abolished ISG15 induction upon stimulation of PBMCs with R848, poly I:C, and CpG A.
Res Sq

2026 Jan 9.
bioRxiv

2025 February 21.
bioRxiv

Loss of JAK1 Function Causes G2/M Cell Cycle Defects Vulnerable to Kif18a Inhibition. [Abstract]

2025 Feb 24:2025.02.19.638911. PMID: 40060568

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (309.21 mM; Need ultrasonic; 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

3.0921 mL

15.4603 mL

30.9205 mL

5 mM

0.6184 mL

3.0921 mL

6.1841 mL

10 mM

0.3092 mL

1.5460 mL

3.0921 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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 (6.43 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (6.43 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (6.43 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: 0.5% CMC-Na/saline water

Solubility: 3.64 mg/mL (11.26 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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (274 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Vazquez ML, et al. Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases. J Med Chem. 2018 Feb 8;61(3):1130-1152. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.0921 mL	15.4603 mL	30.9205 mL	77.3013 mL
	5 mM	0.6184 mL	3.0921 mL	6.1841 mL	15.4603 mL
	10 mM	0.3092 mL	1.5460 mL	3.0921 mL	7.7301 mL
	15 mM	0.2061 mL	1.0307 mL	2.0614 mL	5.1534 mL
	20 mM	0.1546 mL	0.7730 mL	1.5460 mL	3.8651 mL
	25 mM	0.1237 mL	0.6184 mL	1.2368 mL	3.0921 mL
	30 mM	0.1031 mL	0.5153 mL	1.0307 mL	2.5767 mL
	40 mM	0.0773 mL	0.3865 mL	0.7730 mL	1.9325 mL
	50 mM	0.0618 mL	0.3092 mL	0.6184 mL	1.5460 mL
	60 mM	0.0515 mL	0.2577 mL	0.5153 mL	1.2884 mL
	80 mM	0.0387 mL	0.1933 mL	0.3865 mL	0.9663 mL
	100 mM	0.0309 mL	0.1546 mL	0.3092 mL	0.7730 mL

Keywords

Abrocitinib

11 Cited Publications

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Abrocitinib

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Publications Citing Use of MedChemExpress (MCE) Abrocitinib

Ver todos los productos específicos de isoformas JAK

Actividad biológica

Chemical Information

Publications (11)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Abrocitinib Related Classifications

HY-107429 Related Classifications