Cyt387

• CAT Number: I000293
• CAS Number: 1056634-68-4
• Molecular Formula: C₂₃H₂₂N₆O₂
• Molecular Weight: 414.46
• Purity: ≥95%
• Target: JAK
• Solubility: DMSO: ≥ 72.5 mg/mL
• Storage: 3 years -20℃ powder
• IC50: 11 nM/18 nM(JAK1/JAK2) [1]
• IUPAC Name: N-(cyanomethyl)-4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide
• InChI: InChI=1S/C23H22N6O2/c24-10-12-25-22(30)18-3-1-17(2-4-18)21-9-11-26-23(28-21)27-19-5-7-20(8-6-19)29-13-15-31-16-14-29/h1-9,11H,12-16H2,(H,25,30)(H,26,27,28)
• InChIKey: ZVHNDZWQTBEVRY-UHFFFAOYSA-N
• SMILES: C1COCCN1C2=CC=C(C=C2)NC3=NC=CC(=N3)C4=CC=C(C=C4)C(=O)NCC#N

Cyt387 (Cat.No:I000293) is a potent and selective inhibitor of Janus kinase 1 and 2 (JAK1/2). It exhibits anti-inflammatory and immunomodulatory properties, making it a promising candidate for the treatment of various inflammatory and autoimmune diseases. Further studies are underway to explore its therapeutic potential and safety profiles. 

Reference

1:Enhanced Antitumor Activity of Cetuximab in Combination with the Jak Inhibitor CYT387 against Non-Small-Cell Lung Cancer with Various Genotypes. Hu Y, Dong XZ, Liu X, Liu P, Chen YB.Mol Pharm. 2016 Feb 1;13(2):689-97. doi: 10.1021/acs.molpharmaceut.5b00927. Epub 2015 Dec 29. PMID: 26685983 2:P-glycoprotein (MDR1/ABCB1) and breast cancer resistance protein (BCRP/ABCG2) restrict brain accumulation of the JAK1/2 inhibitor, CYT387. Durmus S, Xu N, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.Pharmacol Res. 2013 Oct;76:9-16. doi: 10.1016/j.phrs.2013.06.009. Epub 2013 Jul 1. PMID: 23827160 3:Safety and efficacy of CYT387, a JAK1 and JAK2 inhibitor, in myelofibrosis. Pardanani A, Laborde RR, Lasho TL, Finke C, Begna K, Al-Kali A, Hogan WJ, Litzow MR, Leontovich A, Kowalski M, Tefferi A.Leukemia. 2013 Jun;27(6):1322-7. doi: 10.1038/leu.2013.71. Epub 2013 Mar 5. PMID: 23459451 Free PMC Article4:Liquid chromatography-tandem mass spectrometric assay for the JAK2 inhibitor CYT387 in plasma. Sparidans RW, Durmus S, Xu N, Schinkel AH, Schellens JH, Beijnen JH.J Chromatogr B Analyt Technol Biomed Life Sci. 2012 May 1;895-896:174-7. doi: 10.1016/j.jchromb.2012.03.021. Epub 2012 Mar 23. PMID: 22476054 5:The novel JAK inhibitor CYT387 suppresses multiple signalling pathways, prevents proliferation and induces apoptosis in phenotypically diverse myeloma cells. Monaghan KA, Khong T, Burns CJ, Spencer A.Leukemia. 2011 Dec;25(12):1891-9. doi: 10.1038/leu.2011.175. Epub 2011 Jul 26. PMID: 21788946 6:CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Tyner JW, Bumm TG, Deininger J, Wood L, Aichberger KJ, Loriaux MM, Druker BJ, Burns CJ, Fantino E, Deininger MW.Blood. 2010 Jun 24;115(25):5232-40. doi: 10.1182/blood-2009-05-223727. Epub 2010 Apr 12. PMID: 20385788 Free PMC Article7:CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. Pardanani A, Lasho T, Smith G, Burns CJ, Fantino E, Tefferi A.Leukemia. 2009 Aug;23(8):1441-5. doi: 10.1038/leu.2009.50. Epub 2009 Mar 19. PMID: 19295546