Cat. No.: HY-112708

Brepocitinib

(Synonyms: PF-06700841)

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

Brepocitinib (PF-06700841) is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC₅₀s of 17 nM and 23 nM, respectively. Brepocitinib also inhibits JAK2 and JAK3 with IC₅₀s of 77 nM and 6.49 μM, respectively.

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Pureté: 99.95%
CAS No.: 1883299-62-4
Formule: C₁₈H₂₁F₂N₇O
Masse moléculaire:389.40

Stockage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Brepocitinib Chemical Structure

CAS No.: 1883299-62-4

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

JAK1

17 nM (IC₅₀)

JAK2

77 nM (IC₅₀)

JAK3

6.9 μM (IC₅₀)

Voir tous les produits spécifiques à Isoform JAK :

In Vitro

Brepocitinib (PF-06700841; Compound 23) potently inhibits TYK2/JAK2 mediated IL-12/pSTAT4 and IL-23/pSTAT3 (human whole blood (HWB) IC₅₀s of 65 and 120 nM, respectively)^[1].
Brepocitinib has good potency against IL6/pStat1 in the CD3⁺ cellular subset (IC₅₀ of 81 nM), but lower inhibition of IL6/pSTAT3, again in the CD3⁺ cellular subset (IC₅₀ of 641 nM)^[1].
Brepocitinib also inhibits the JAK1/JAK3 driven γ-common chain cytokines, represented by IL-15/pStat5 and IL-21/pSTAT3 with reasonable potency (HWB IC₅₀s of 238 and 204 nM, respectively)^[1].
Brepocitinib inhibits EPO/pSTAT5 (JAK2 homodimer) in HWB spiked with CD34⁺ progenitor cells (IC₅₀ of 577 nM). IL10/pSTAT3 (TYK2/JAK1) and IL27/pSTAT3 (JAK1/JAK2/TYK2) are also inhibited by Brepocitinib with IC₅₀s of 305 nM and 86 nM, respectively^[1].

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

In Vivo

Brepocitinib (PF-06700841; Compound 23; 3-30 mg/kg; oral administration; for 7 consecutive days; female Lewis rats) treatment significantly reduces paw volume increase in a dose-dependent manner. The plasma concentrations in animals dosed with Brepocitinib at peak (30 min) and trough (24 h) time intervals post final dose respectively are as follows: 3 mg/kg, 3.54 μM, 0.0221 μM; 10 mg/kg, 10.95 μM, 0.06 μM; and 30 mg/kg, 23.89 μM, 0.06 μM^[1].

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

Animal Model:

Female Lewis rats with induced arthritis^[1]
Dosage:

3 mg/kg, 10 mg/kg, or 30 mg/kg
Administration:

Oral administration; for 7 consecutive days
Result:

Increased in paw volume was significantly lower and dose-dependent.

Chemical Information

CAS No. 1883299-62-4
Appearance Solid
Masse moléculaire 389.40
Formule C₁₈H₂₁F₂N₇O
Color White to light yellow
SMILES

O=C([C@H]1C(F)(F)C1)N2C3CN(C4=NC(NC5=CN(C)N=C5)=NC=C4)CC2CC3
Synonyms

PF-06700841
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (3)

All RT-PCRWBCell Proliferation/Viability AssayCell Migration/Invasion Assay

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Journal Impact Factor

J Exp Clin Cancer Res

Unveiling the role of HP1α-HDAC1-STAT1 axis as a therapeutic target for HP1α-positive intrahepatic cholangiocarcinoma. [Abstract]

2024 May 30;43(1):152. PMID: 38812060

Brepocitinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2024 May 30;43(1):152. [Abstract]

Brepocitinib (PF-06700841; 50 nM; 24 h) inhibited mRNA expression of p-STAT1, STAT1, and ISG expression by HP1α knockdown in HUCCT1 and HCCC-9810 cells.

Brepocitinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2024 May 30;43(1):152. [Abstract]

Brepocitinib (PF-06700841; 50 nM; 24 h) inhibited protein expression of p-STAT1, STAT1, and ISG by HP1α knockdown in HUCCT1 and HCCC-9810 cells.
Inflamm Bowel Dis

Clinical and Mechanistic Characteristics of Current JAK Inhibitors in IBD. [Abstract]

2021 Oct 18;27(10):1674-1683. PMID: 33295611
Heliyon

Hyperin promotes proliferation, migration, and invasion of HTR-8/SVneo trophoblast cells via activation of JAK1/STAT3 pathway in recurrent spontaneous abortions. [Abstract]

2023 Jan 13;9(1):e12958. PMID: 36747955

Brepocitinib purchased from MedChemExpress. Usage Cited in: Heliyon. 2023 Jan 13;9(1):e12958. [Abstract]

PF-06700841 (Brepocitinib; 20 nM; 24 h) blocks hyperin-induced expression of JAK1 and STAT3 in HTR-8/SVneo cells.

Brepocitinib purchased from MedChemExpress. Usage Cited in: Heliyon. 2023 Jan 13;9(1):e12958. [Abstract]

Brepocitinib (PF-06700841; 20 nM; 24 h) blocked hyperin induced JAK1 and STAT3 mRNA expression in HTR8/SVneo cells.

Brepocitinib purchased from MedChemExpress. Usage Cited in: Heliyon. 2023 Jan 13;9(1):e12958. [Abstract]

Brepocitinib (PF-06700841; 20 nM; 12, 24, 36, 48 h) blocked the effects of hyperin on cell proliferation in HTR8/SVneo cells.

Brepocitinib purchased from MedChemExpress. Usage Cited in: Heliyon. 2023 Jan 13;9(1):e12958. [Abstract]

Brepocitinib (PF-06700841; 20 nM; 12, 24, 36, 48 h) blocked the protein expression of Ki67, MCM2, MMP2, MMP9, VEGFA, and PCNA in HTR8/SVneo cells.

Brepocitinib purchased from MedChemExpress. Usage Cited in: Heliyon. 2023 Jan 13;9(1):e12958. [Abstract]

Brepocitinib (PF-06700841; 20 nM; 48 h) inhibited the effect of hyperin on HTR-8/SVneo cell migration.

Brepocitinib purchased from MedChemExpress. Usage Cited in: Heliyon. 2023 Jan 13;9(1):e12958. [Abstract]

Brepocitinib (PF-06700841; 20 nM; 48 h) inhibited the invasion ability in HTR-8/SVneo cells.

Solvant et solubilité

In Vitro:

DMSO : 125 mg/mL (321.01 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

2.5681 mL

12.8403 mL

25.6805 mL

5 mM

0.5136 mL

2.5681 mL

5.1361 mL

10 mM

0.2568 mL

1.2840 mL

2.5681 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (274 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 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)
Instruction de manipulation (2659 KB)

Références

[1]. Fensome A, et al. Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841). J Med Chem. 2018 Oct 11;61(19):8597-8612. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5681 mL	12.8403 mL	25.6805 mL	64.2013 mL
	5 mM	0.5136 mL	2.5681 mL	5.1361 mL	12.8403 mL
	10 mM	0.2568 mL	1.2840 mL	2.5681 mL	6.4201 mL
	15 mM	0.1712 mL	0.8560 mL	1.7120 mL	4.2801 mL
	20 mM	0.1284 mL	0.6420 mL	1.2840 mL	3.2101 mL
	25 mM	0.1027 mL	0.5136 mL	1.0272 mL	2.5681 mL
	30 mM	0.0856 mL	0.4280 mL	0.8560 mL	2.1400 mL
	40 mM	0.0642 mL	0.3210 mL	0.6420 mL	1.6050 mL
	50 mM	0.0514 mL	0.2568 mL	0.5136 mL	1.2840 mL
	60 mM	0.0428 mL	0.2140 mL	0.4280 mL	1.0700 mL
	80 mM	0.0321 mL	0.1605 mL	0.3210 mL	0.8025 mL
	100 mM	0.0257 mL	0.1284 mL	0.2568 mL	0.6420 mL

Keywords

Brepocitinib

3 Cited Publications

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Brepocitinib

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Orally Active Compound Library

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Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Anti-Liver Cancer Compound Library

Rare Diseases Drug Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Autoimmune Disease Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Brepocitinib

Voir tous les produits spécifiques à Isoform JAK

Activité biologique

Chemical Information

Publications (3)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Brepocitinib Related Classifications

HY-112708 Related Classifications