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Baricitinib phosphate

Catalog No.GC13830

A JAK1 and JAK2 inhibitor

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Baricitinib phosphate Chemical Structure

Cas No.: 1187595-84-1

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5mg
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$63.00
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50mg
$189.00
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200mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

For the determination of IL-6-induced MCP-1 production, PBMCs are plated at 3.3×105 cells per well in RPMI 1640+10% FCS in the presence or absence of various concentrations of INCB028050 (1 nM, 10 nM, 100 nM, 1 μM, and 10 μM). Following preincubation with compound for 10 min at room temperature, cells are stimulated by adding 10 ng/mL human recombinant IL-6 to each well. Cells are incubated for 48 h at 37°C, 5% CO2. Supernatants are harvested and analyzed by ELISA for levels of human MCP-1. The ability of INCB028050 to inhibit IL-6-induced secretion of MCP-1 is reported as the concentration required for 50% inhibition (IC50). Proliferation of Ba/F3-TEL-JAK3 cells is performed over 3 d using Cell-Titer Glo[1].

Animal experiment:

Rats[1] Female rats (n=6 per gender per group) are given a dose of 10 mg/kg Baricitinib and given by oral gavage at 10 mL/kg. The first three rats are bled at 0 (predose), 2, 8, and 24 h, and the second three rats are bled 1, 4, and 12 h after dosing. EDTA is used as the anticoagulant, and samples are centrifuged to obtain plasma. An analytical method for the quantification of INCB028050 has been developed and used to analyze samples from toxicology studies. The method combines a protein precipitation extraction with 10% methanol in acetonitrile and LC/MS/MS analysis. The method has demonstrated a linear assay range 1-5000 nM using 0.1 mL of study samples. Data are processed using Analyst 1.3.1. A standard curve is determined from peak area ratio versus concentration using a weighted linear regression (1/x2). Mice[2] The C3H/HeJ graft-recipient mouse model of AA is used for these experiments. Briefly, alopecic skin from a C3H/HeJ mouse that spontaneously developed hair loss is grafted onto 8-10 week old C3H/HeJ mice free of disease. At the time of grafting, an osmotic pump that administered approximately 0.7 mg/day of Baricitinib or placebo is implanted. Osmotic pumps are changed monthly. A time-to-event survival analysis for interval censored data is performed. The survival and interval packages in R are used to perform log-rank tests. The hypothesis that the survival distributions are equal in the (n=10) Baricitinib-treated mice and (n=10) placebo-treated mice is rejected at the 5% level using Sun's score to perform an exact log-rank two-sample test with the p-value of 0.0035.

References:

[1]. Fridman JS, et al. Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J Immunol. 2010 May 1;184(9):5298-307.
[2]. Jabbari A, et al. Reversal of Alopecia Areata Following Treatment With the JAK1/2 Inhibitor Baricitinib. EBioMedicine. 2015 Feb 26;2(4):351-5.

Background

Direct and indirect inhibition of the JAKs has demonstrated rapid and sustained improvement in clinical measures of disease. Baricitinib phosphate (INCB 028050) is a selective JAK1 and JAK2 inhibitor.

In vitro: Baricitinib phosphate is a selective orally bioavailable JAK1/JAK2 inhibitor with nanomolar potency against JAK1 (5.9 nM) and JAK2 (5.7 nM) and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. INCB028050 inhibits intracellular signaling of multiple proinflammatory cytokines including IL-6 and IL-23 at concentrations, 50 nM [1].

In vivo: Significant efficacy was achieved in the rat adjuvant arthritis model with doses of Baricitinib phosphate providing partial and/or periodic inhibition of JAK1/JAK2 and no inhibition of JAK3. Baricitinib phosphate was also effective in multiple murine models of arthritis, with no evidence of suppression of humoral immunity or adverse hematologic effects [2].

Clinical trial: Several clinical trials have been conducted to investigated the PK, efficacy and DDI of Baricitinib phosphate in healthy people as well as in participants With Rheumatoid Arthritis.

Reference:
[1] Fridman JS, Scherle PA, Collins R, Burn TC, Li Y, Li J, Covington MB, Thomas B, Collier P, Favata MF, Wen X, Shi J, McGee R, Haley PJ, Shepard S, Rodgers JD, Yeleswaram S, Hollis G, Newton RC, Metcalf B, Friedman SM, Vaddi K.  Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J Immunol. 2010;184(9):5298-307.

Chemical Properties

Cas No. 1187595-84-1 SDF
Chemical Name 2-[1-ethylsulfonyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile;phosphoric acid
Canonical SMILES CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3.OP(=O)(O)O
Formula C16H20N7O6PS M.Wt 469.41
Solubility ≥ 172.6 mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.1303 mL 10.6517 mL 21.3033 mL
5 mM 0.4261 mL 2.1303 mL 4.2607 mL
10 mM 0.213 mL 1.0652 mL 2.1303 mL
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