For research use only. Not for therapeutic Use.
NVP-BSK805 (Cat No.: I000383) is a potent and selective inhibitor of Janus kinase 2 (JAK2) with an IC₅₀ of 0.5 nM. It exhibits high selectivity over other JAK family kinases, including JAK1, JAK3, and TYK2. NVP-BSK805 has been widely used in cancer and inflammatory disease research, particularly in studying myeloproliferative disorders driven by JAK2 mutations. By targeting JAK2-mediated signaling pathways, it provides insights into therapeutic strategies for conditions such as polycythemia vera, essential thrombocythemia, and myelofibrosis.
CAS Number | 1092499-93-8 |
Synonyms | 4-[[2,6-difluoro-4-[3-(1-piperidin-4-ylpyrazol-4-yl)quinoxalin-5-yl]phenyl]methyl]morpholine;dihydrochloride |
Molecular Formula | C27H28F2N6O |
Purity | ≥95% |
Target | Stem Cell/Wnt |
Solubility | DMSO 67 mg/mL; Water <1 mg/mL; Ethanol 7 mg/mL |
Storage | Store at -20°C |
IC50 | 0.48 ± 0.02 nM (JAK2 JH1); 0.58 ± 0.03 nM (FL JAK2 wt) [1] |
IUPAC Name | 4-[[2,6-difluoro-4-[3-(1-piperidin-4-ylpyrazol-4-yl)quinoxalin-5-yl]phenyl]methyl]morpholine |
InChI | 1S/C27H28F2N6O/c28-23-12-18(13-24(29)22(23)17-34-8-10-36-11-9-34)21-2-1-3-25-27(21)33-26(15-31-25)19-14-32-35(16-19)20-4-6-30-7-5-20/h1-3,12-16,20,30H,4-11,17H2 |
InChIKey | IBPVXAOOVUAOKJ-UHFFFAOYSA-N |
SMILES | C1CNCCC1N2C=C(C=N2)C3=NC4=C(C=CC=C4N=C3)C5=CC(=C(C(=C5)F)CN6CCOCC6)F |
Reference | </br>1:Effects of Jak2 type 1 inhibitors NVP-BSK805 and NVP-BVB808 on Jak2 mutation-positive and Bcr-Abl-positive cell lines. Ringel F, Kaeda J, Schwarz M, Oberender C, Grille P, Dörken B, Marque F, Manley PW, Radimerski T, le Coutre P.Acta Haematol. 2014;132(1):75-86. doi: 10.1159/000356784. Epub 2014 Jan 31. PMID: 24504330 </br>2:Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805. Baffert F, Régnier CH, De Pover A, Pissot-Soldermann C, Tavares GA, Blasco F, Brueggen J, Chène P, Drueckes P, Erdmann D, Furet P, Gerspacher M, Lang M, Ledieu D, Nolan L, Ruetz S, Trappe J, Vangrevelinghe E, Wartmann M, Wyder L, Hofmann F, Radimerski T.Mol Cancer Ther. 2010 Jul;9(7):1945-55. doi: 10.1158/1535-7163.MCT-10-0053. Epub 2010 Jun 29. PMID: 20587663 Free Article |
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