CEP-33779

• CAT Number: I001033
• CAS Number: 1257704-57-6
• Molecular Formula: C24H26N6O2S
• Molecular Weight: 462.6
• Purity: ≥95%
• Target: JAK
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 1.8 nM
• IUPAC Name: N-[3-(4-methylpiperazin-1-yl)phenyl]-8-(4-methylsulfonylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine
• InChI: InChI=1S/C24H26N6O2S/c1-28-13-15-29(16-14-28)20-6-3-5-19(17-20)25-24-26-23-22(7-4-12-30(23)27-24)18-8-10-21(11-9-18)33(2,31)32/h3-12,17H,13-16H2,1-2H3,(H,25,27)
• InChIKey: RFZKSQIFOZZIAQ-UHFFFAOYSA-N
• SMILES: CN1CCN(CC1)C2=CC=CC(=C2)NC3=NN4C=CC=C(C4=N3)C5=CC=C(C=C5)S(=O)(=O)C

CEP-33779（Cat No.:I001033） is a novel inhibitor that selectively targets Janus kinase 2 (JAK2). It is orally bioavailable, meaning it can be taken by mouth and absorbed into the bloodstream. CEP-33779 demonstrates potent inhibitory activity against JAK2, with an IC50 (half-maximal inhibitory concentration) value of 1.8 nM. By inhibiting JAK2, CEP-33779 interferes with signaling pathways involved in cellular processes and immune responses. This compound holds promise for potential therapeutic applications in conditions where JAK2 dysregulation plays a role, such as certain types of cancers and inflammatory disorders.

Reference

1:CEP-33779 antagonizes ATP-binding cassette subfamily B member 1 mediated multidrug resistance by inhibiting its transport function. Tang SJ, Chen LK, Wang F, Zhang YK, Huang ZC, To KK, Wang XK, Talele TT, Chen ZS, Chen WQ, Fu LW.Biochem Pharmacol. 2014 Sep 15;91(2):144-56. doi: 10.1016/j.bcp.2014.07.008. Epub 2014 Jul 21. PMID: 25058526 2:A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779. Dugan BJ, Gingrich DE, Mesaros EF, Milkiewicz KL, Curry MA, Zulli AL, Dobrzanski P, Serdikoff C, Jan M, Angeles TS, Albom MS, Mason JL, Aimone LD, Meyer SL, Huang Z, Wells-Knecht KJ, Ator MA, Ruggeri BA, Dorsey BD.J Med Chem. 2012 Jun 14;55(11):5243-54. doi: 10.1021/jm300248q. Epub 2012 May 18. PMID: 22594690 3:Therapeutic efficacy of CEP-33779, a novel selective JAK2 inhibitor, in a mouse model of colitis-induced colorectal cancer. Seavey MM, Lu LD, Stump KL, Wallace NH, Hockeimer W, O/’Kane TM, Ruggeri BA, Dobrzanski P.Mol Cancer Ther. 2012 Apr;11(4):984-93. doi: 10.1158/1535-7163.MCT-11-0951. Epub 2012 Feb 14. PMID: 22334590 Free Article4:Depletion of autoreactive plasma cells and treatment of lupus nephritis in mice using CEP-33779, a novel, orally active, selective inhibitor of JAK2. Lu LD, Stump KL, Wallace NH, Dobrzanski P, Serdikoff C, Gingrich DE, Dugan BJ, Angeles TS, Albom MS, Mason JL, Ator MA, Dorsey BD, Ruggeri BA, Seavey MM.J Immunol. 2011 Oct 1;187(7):3840-53. doi: 10.4049/jimmunol.1101228. Epub 2011 Aug 31. PMID: 21880982 Free Article5:A highly selective, orally active inhibitor of Janus kinase 2, CEP-33779, ablates disease in two mouse models of rheumatoid arthritis. Stump KL, Lu LD, Dobrzanski P, Serdikoff C, Gingrich DE, Dugan BJ, Angeles TS, Albom MS, Ator MA, Dorsey BD, Ruggeri BA, Seavey MM.Arthritis Res Ther. 2011 Apr 21;13(2):R68. doi: 10.1186/ar3329. PMID: 21510883 Free PMC Article