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Angiogenesis JAK Baricitinib

Baricitinib

Catalog No. T2485   CAS 1187594-09-7
Synonyms: LY3009104, INCB028050
Purity 100.00% Datasheet MSDS

Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities.

Baricitinib, CAS 1187594-09-7
Pack Size Availability Price/USD Quantity
1 mg In stock 33.00
2 mg In stock 43.00
5 mg In stock 69.00
10 mg In stock 80.00
25 mg In stock 107.00
50 mg In stock 134.00
100 mg In stock 167.00
200 mg In stock 217.00
1 mL * 10 mM (in DMSO) In stock 76.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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Description Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities.
Targets&IC50 Chk2 :ic50 >1μM,   JAK1 :ic50 5.9nM,   JAK2 :ic50 5.7nM,   JAK3 :ic50 >400nM,   Tyk2 :ic50 53nM,  
Kinase Assay Enzyme assays are performed using a homogeneous time-resolved fluorescence assay with recombinant epitope tagged kinase domains (JAK1, 837-1142; JAK2, 828-1132; JAK3, 718-1124; Tyk2, 873-1187) or full-length enzyme (cMET and Chk2) and peptide substrate. Each enzyme reaction is performed with or without test compound (11-point dilution), JAK, cMET, or Chk2 enzyme, 500 nM (100 nM for Chk2) peptide, ATP (at the Km specific for each kinase or 1 mM), and 2.0% DMSO in assay buffer. The calculated IC50 value is the compound concentration required for inhibition of 50% of the fluorescent signal. Additional kinase assays are performed at Cerep using standard conditions at 200 nM. Enzymes tested included: Abl, Akt1, AurA, AurB, CDC2, CDK2, CDK4, CHK2, c-kit, EGFR, EphB4, ERK1, ERK2, FLT-1, HER2, IGF1R, IKKα, IKKβ, JNK1, Lck, MEK1, p38α, p70S6K, PKA, PKCα, Src, and ZAP70[1].
Cell Research
Baricitinib(INCB 028050) is dissolved in stock solutions, and then diluted with appropriate media before use[1]. Human PBMCs are isolated by leukapheresis followed by Ficoll-Hypaque centrifugation. 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 Research
Animal Model: Collagen-induced arthritis (CIA) mice
Synonyms LY3009104, INCB028050
Purity 100.00%
Appearance solid
Molecular Weight 371.42
Formula C16H17N7O2S
CAS No. 1187594-09-7

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 69 mg/mL (185.8 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL

Citations

References and Literature
1. Fridman JS, et al. J Immunol, 2010, 184(9), 5298-5307. 2. Kontzias A, et al. Curr Opin Pharmacol, 2012, 12(4), 464-470. 3. Norman P, et al. Expert Opin Ther Pat, 2012, 22(10), 1233-1249. 4. Norman P, et al. Expert Opin Ther Pat, 2012, 22(9), 1105-1109. 5. Khan IM, et al. Intermuscular and perimuscular fat expansion in obesity correlates with skeletal muscle T cell and macrophage infiltration resistance. Int J Obes (Lond). 2015 Nov;39(11):1607-18.

Related Compound Libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Stem cell Differentiation Compound Library Epigenetics Compound Library Tyrosine kinase inhibitor library FDA-approved Drug Library Immunology/Inflammation Compound Library Kinase Inhibitor Library Anti-cancer Approved drug Library Angiogenesis related Compound Library JAK STAT Compound Library Cell cycle related Compound Library

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