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HER2&FLT3

Baricitinib (LY3009104, INCB028050) (1187594-09-7)

Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Phase 3.

Not Intended for Therapeutic Use. For research use only.

CAS: 1187594-09-7 Category

Baricitinib (LY3009104, INCB028050) (1187594-09-7) Description:

Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities. Upon administration, baricitinib binds to JAK1/2, which inhibits JAK1/2 activation and leads to the inhibition of the JAK-signal transducers and activators of transcription (STAT) signaling pathway. This decreases the production of inflammatory cytokines and may prevent an inflammatory response. In addition, baricitinib may induce apoptosis and reduce proliferation of JAK1/2-expressing tumor cells. JAK kinases are intracellular enzymes involved in cytokine signaling, inflammation, immune function and hematopoiesis; they are also upregulated and/or mutated in various tumor cell types.

Baricitinib (LY3009104, INCB028050) (1187594-09-7) Specifications:

Product Name Baricitinib (LY3009104, INCB028050)
Synonym INCB-028050; INCB-28050; INCB 28050; INCB28050; LY-3009104; LY 3009104; LY3009104; Baricitinib Phosphate.
Chemical Name 2-[1-ethylsulfonyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile
Purity ≥98% (HPLC)
CAS Number 1187594-09-7
Molecular Formula C16H17N7O2S
Molecular Weight 371.4
Monoisotopic Mass 371.419 g/mol
MDL number N/A
InChIKey FBPOWTFFUBBKBB-UHFFFAOYSA-N
InChi Code InChI=1S/C16H17N7O2S.H3O4P/c1-2-26(24,25)22-9-16(10-22,4-5-17)23-8-12(7-21-23)14-13-3-6-18-15(13)20-11-19-14;1-5(2,3)4/h3,6-8,11H,2,4,9-10H2,1H3,(H,18,19,20);(H3,1,2,3,4)
SMILES CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3
Form Solid powder
Color Yellow
Solubility  Soluble in DMSO
Storage Temp.  0 – 4 C for short term (days to weeks), or -20 C for long term (months).
Shelf life >2 years if stored properly
Handling Protect from air and light
Application JAK Inhibitor

 


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RIDADR NONH for all modes of transport

References:

  • Nakayamada S, Kubo S, Iwata S, Tanaka Y. Recent Progress in JAK Inhibitors for the Treatment of Rheumatoid Arthritis. BioDrugs. 2016 Aug 31. [Epub ahead of print] Review. PubMed PMID: 27577235.
  • Roskoski R Jr. Janus kinase (JAK) inhibitors in the treatment of inflammatory and neoplastic diseases. Pharmacol Res. 2016 Jul 26;111:784-803. doi: 10.1016/j.phrs.2016.07.038. [Epub ahead of print] Review. PubMed PMID: 27473820.
  • Kubo S, Nakayamada S, Tanaka Y. Baricitinib for the treatment of rheumatoid arthritis. Expert Rev Clin Immunol. 2016 Sep;12(9):911-9. doi: 10.1080/1744666X.2016.1214576. Epub 2016 Aug 5. PubMed PMID: 27427830.
  • Tanaka Y. [Tofacitinib for the treatment of rheumatoid arthritis]. Nihon Rinsho. 2016 Jun;74(6):974-80. Review. Japanese. PubMed PMID: 27311188.
  • Perez-Gomez MV, Sanchez-Niño MD, Sanz AB, Zheng B, Martín-Cleary C, Ruiz-Ortega M, Ortiz A, Fernandez-Fernandez B. Targeting inflammation in diabetic kidney disease: early clinical trials. Expert Opin Investig Drugs. 2016 Sep;25(9):1045-58. doi: 10.1080/13543784.2016.1196184. Epub 2016 Jun 13. PubMed PMID: 27268955.

1 review for Baricitinib (LY3009104, INCB028050) (1187594-09-7)

  1. Cofttek

    Never had such good experience before,The Baricitinib (LY3009104, INCB028050) (1187594-09-7) is high purity,also customer service is pretty nice !gotta try!!

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