1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK

Peficitinib (Synonyms: ASP015K; JNJ-54781532)

Cat. No.: HY-19568 Purity: 99.43%
Handling Instructions

Peficitinib is an oral JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.

For research use only. We do not sell to patients.

Peficitinib Chemical Structure

Peficitinib Chemical Structure

CAS No. : 944118-01-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
25 mg USD 384 In-stock
Estimated Time of Arrival: December 31
50 mg USD 708 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1188 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

View All JAK Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Peficitinib is an oral JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.

IC50 & Target[1]

JAK3

0.7 nM (IC50)

JAK1

3.9 nM (IC50)

Tyk2

4.8 nM (IC50)

JAK2

5 nM (IC50)

In Vitro

Peficitinib is an oral JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. Peficitinib inhibits IL-2-induced T cell proliferation with an IC50 of 10 nM. Peficitinib also suppresses the IL-2-induced STAT5 phosphorylation in rat and human whole blood, with mean IC50s of 124 nM and 127 nM, respectively[1].

In Vivo

Peficitinib (20 mg/kg, p.o.) suppresses IL-2-induced STAT5 phosphorylation by 78% in the rat model of adjuvant-induced arthritis (AIA). Peficitinib potently inhibits the increase in paw volume (≥1 mg/kg) with an ED50 of 2.7 mg/kg, significantly reduces the bone destruction score (≥10 mg/kg) and almost fully ameliorates both paw swelling and bone destruction scores (30 mg/kg)[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 60 mg/mL (183.83 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0638 mL 15.3191 mL 30.6382 mL
5 mM 0.6128 mL 3.0638 mL 6.1276 mL
10 mM 0.3064 mL 1.5319 mL 3.0638 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

Human JAK1, JAK2, JAK3, TYK2-domains assays performed using streptavidin-coated 96-well plates. Reaction mixture contained 15 mM Tris-HCl (pH 7.5), 0.01% Tween 20, 2 mM dithiothreitol, 10 mM MgCl2, 250 nM Biotin-Lyn-Substrate-2 (for JAK1, 2 and 3) or Biotin-IRS1-Substrate (for TYK2), and ATP (at final concentrations of 200 μM [JAK1], 10 μM [JAK2], 8 μM [JAK3], and 4 μM [TYK2]). Peficitinib or tofacitinib is dissolved in DMSO. The reaction is initiated by adding the kinase domain, followed by incubation at room temperature for 1 h. Kinase activity is measured as the rate of phosphorylation of Biotin-Lyn-Substrate-2 or Biotin-IRS-Substrate using HRP-conjugated anti-phosphotyrosine antibody (HRP-PY-20) using a phosphotyrosine-specific ELISA. TYK2 kinase assay of Peficitinib is performed with the ATP concentration of 10 μM[1].

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

Cell Assay
[1]

Splenocytes from male Lewis rats are suspended in RPMI1640 supplemented with 10% fetal bovine serum and 50 μM 2-mercaptoethanol at a density of 1.5 × 106 cells/mL. Rat splenocytes are cultured with Concanavalin A for 24 h at 37°C to induce IL-2 receptor expression. Splenocytes are then incubated with IL-2 and Peficitinib or tofacitinib at designated concentrations in 96-well tissue culture plates. After 3-day incubation, alamarBlue® is added to each of the test wells, followed by 4-6 h incubation. Fluorescence intensity is measured at an excitation wavelength of 545 nm and an emission wavelength of 590 nm. All experiments are performed in triplicate, and experiments are performed either four times or once for assays using Peficitinib or tofacitinib, respectively. For each individual, wells cultured with cells and medium alone are prepared for the blanks, and IL-2 stimulated cells without JAK inhibitors are prepared for the controls. To calculate the % inhibition of JAK inhibitors, blanks and controls are designated as 100% and 0% inhibition, respectively[1].

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

Animal Administration
[1]

Rats[1]
Seven-weeks-old female Lewis rats are used for the adjuvant-induced arthritis (AIA) model. Body weight and left hind paw volume of each rat are measured (MK-101PR volume meter), and the values are used to assign animals to one of six groups (n = 10). Arthritis is induced on day 0 in five of these groups by injecting a suspension of Mycobacterium tuberculosis H37 RA strain (0.5 mg/rat) in liquid paraffin into the right hind foot pad. The remaining group is not injected with adjuvant (normal group, n = 10). For the oral administration regimen, four of the adjuvant-injected groups receive Peficitinib (1, 3, 10, and 30 mg/kg) dissolved in 0.5% methylcellulose (MC) once daily. Rats in the normal and control groups receive 0.5% MC alone[1].

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

References
Molecular Weight

326.39

Formula

C₁₈H₂₂N₄O₂

CAS No.

944118-01-8

SMILES

O[[email protected]](C[[email protected]@H]1C[[email protected]]2C3)(C2)C[[email protected]@H]3[[email protected]]1NC4=C5C(NC=C5)=NC=C4C(N)=O

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

Room temperature in continental US; may vary elsewhere

Purity: 99.43%

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Peficitinib
Cat. No.:
HY-19568
Quantity:

Peficitinib

Cat. No.: HY-19568