NVP BSK 805
Chemical Name: 8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline trihydrochloride
Purity: ≥98%
Biological Activity
NVP BSK 805 is a potent JAK2 inhibitor (IC50 = 0.48 nM). Exhibits >20-fold selectivity for JAK2 over TYK2, JAK3 and JAK1 (IC50 values are 10.8, 18.7 and 31.6 nM, respectively). Inhibits proliferation and induces apoptosis of JAK2V617F-bearing acute myeloid leukemia cells in vitro and in vivo. Also inhibits erythropoietin-induced polycythemia. Orally bioavailable.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805.
Baffert et al.
Mol.Cancer Ther., 2010;9:1945 -
Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.
Pissot-Soldermann et al.
Bioorg.Med.Chem.Lett., 2010;20:2609
Product Datasheets
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