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Peficitinb (ASP015K, JNJ-54781532)

JAK inhibitor CAS# 944118-01-8

Peficitinb (ASP015K, JNJ-54781532)

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Peficitinb (ASP015K, JNJ-54781532): 5mg $115 In Stock
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Chemical structure

Peficitinb (ASP015K, JNJ-54781532)

3D structure

Chemical Properties of Peficitinb (ASP015K, JNJ-54781532)

Cas No. 944118-01-8 SDF Download SDF
PubChem ID 57928403 Appearance Powder
Formula C18H22N4O2 M.Wt 326.39
Type of Compound N/A Storage Desiccate at -20°C
Synonyms ASP015K; JNJ-54781532
Solubility DMSO : ≥ 60 mg/mL (183.83 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 4-[[(1R,3S)-5-hydroxy-2-adamantyl]amino]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
SMILES C1C2CC3CC(C2)(CC1C3NC4=C5C=CNC5=NC=C4C(=O)N)O
Standard InChIKey DREIJXJRTLTGJC-JQCLMNFQSA-N
Standard InChI InChI=1S/C18H22N4O2/c19-16(23)13-8-21-17-12(1-2-20-17)15(13)22-14-10-3-9-4-11(14)7-18(24,5-9)6-10/h1-2,8-11,14,24H,3-7H2,(H2,19,23)(H2,20,21,22)/t9?,10-,11+,14?,18?
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Peficitinb (ASP015K, JNJ-54781532)

DescriptionPeficitinib 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.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].

References:
[1]. Ito M, et al. A novel JAK inhibitor, peficitinib, demonstrates potent efficacy in a rat adjuvant-induced arthritis model. J Pharmacol Sci. 2017 Jan;133(1):25-33.

Protocol

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].

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].

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].

References:
[1]. Ito M, et al. A novel JAK inhibitor, peficitinib, demonstrates potent efficacy in a rat adjuvant-induced arthritis model. J Pharmacol Sci. 2017 Jan;133(1):25-33.

Peficitinb (ASP015K, JNJ-54781532) Dilution Calculator

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Preparing Stock Solutions of Peficitinb (ASP015K, JNJ-54781532)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.0638 mL 15.3191 mL 30.6382 mL 61.2764 mL 76.5955 mL
5 mM 0.6128 mL 3.0638 mL 6.1276 mL 12.2553 mL 15.3191 mL
10 mM 0.3064 mL 1.5319 mL 3.0638 mL 6.1276 mL 7.6595 mL
50 mM 0.0613 mL 0.3064 mL 0.6128 mL 1.2255 mL 1.5319 mL
100 mM 0.0306 mL 0.1532 mL 0.3064 mL 0.6128 mL 0.766 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Peficitinb (ASP015K, JNJ-54781532)

Peficitinib (ASP015K) is an oral Janus kinase (JAK) inhibitor. It inhibits enzyme activities of JAK1, JAK2, JAK3 and Tyk2 with IC50 values of 3.9, 5.0, 0.71 and 4.8 nmol/L, respectively. It showed moderate selectivity for JAK3 inhibition [1].

JAK family of non-receptor protein tyrosine kinases includes JAK1, JAK2, JAK3 and tyrosine kinase 2 (Tyk2). JAK1, JAK2, JAK3 and Tyk2 are critically important in haematopoietic cells and immune cells [1].

Erythropoietin regulates haematopoiesis (the production of blood cells) [2]. Treatment with ASP015K inhibited the human T-cell proliferation induced by IL-2. And this effect was greater than the effect to inhibit EPO-induced human erythroleukemia cell proliferation. In human whole blood, ASP015K concentration-dependently inhibited STAT5 phosphorylation (pSTAT5) [3].

In healthy volunteers, STAT5-P was dose-dependently inhibited by ASP015K. When the doses of ASP015K were 60, 120, 200, or 300 mg, the mean peak percentage inhibitions of STAT5-P were 84%, 85%, 92%, and 93%, respectively. Plasma ASP015K inhibited STAT5-P with an EC50 value of 48 ng/mL, a shape factor (γ) of ~1.2, and an estimated Emax close to 100%. On days 1, 7, and 14, at ~2 hours after treatment with ASP015K at multiple doses, the peak of median percentage of STAT5-P inhibition appeared [4].

References:
[1].  Takeuchi T, Tanaka Y, Iwasaki M, et al. Efficacy and safety of the oral Janus kinase inhibitor peficitinib (ASP015K) monotherapy in patients with moderate to severe rheumatoid arthritis in Japan: a 12-week, randomised, double-blind, placebo-controlled phase IIb study. Annals of the rheumatic diseases, 2015: annrheumdis-2015-208279.
[2].  Digicaylioglu M, Lipton SA. Erythropoietin-mediated neuroprotection involves cross-talk between Jak2 and NF-κB signalling cascades. Nature, 2001, 412(6847): 641-647.
[3].  Yamazaki S, Morio H, Inami M, et al. THU0101 ASP015K: A Novel Jak Inhibitor Demonstrated Potent Efficacy in Adjuvant-Induced Arthritis Model in Rats. Annals of the Rheumatic Diseases, 2013, 72(Suppl 3): A197-A197.
[4].  Zhu T, Valluri U, Lewand M, et al. THU0256 Pharmacodynamics of ASP015K, A Novel Janus Kinase Inhibitor, in Healthy Volunteers. Annals of the Rheumatic Diseases, 2013, 72(Suppl 3): A252-A252.

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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.

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