Cat. No. Name Size Price Add Cart
KI3702NVP-BSK805 dihydrochloride5 mg$460
NVP-BSK805 dihydrochloride10 mg$630
NVP-BSK805 dihydrochloride50 mg$1650
NVP-BSK805 dihydrochloride200 mg$4540

Chemical Characteristic

Product NameNVP-BSK805 dihydrochloride
CAS No.1092499-93-8
Molecular Weight 563.47
FormulaC27H28F2N6O
Chemical Name8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline
Smilesn1c(cnc2cccc(c12)c1cc(c(c(c1)F)CN1CCOCC1)F)c1cnn(c1)C1CCNCC1
Chemical Structure

Biological activities

NVP-BSK805 can potently suppress JAK2 with IC50 of 0.5 nM, and displays more than 20-fold selectivity towards JAK1, JAK3, and TYK2. NVP-BSK805 shows inhibition to JAK2V617F and JAK2 wild-type with IC50 of 0.5 nM [1]. For cell lines, NVP-BSK805 inhibits JAK2V617F cells (Ba/F3) growth and induces cell apoptosis. NVP-BSK805 also can potently inhibit STAT5 [2]. By inducing activation of caspase cascades, NVP-BSK805 triggered cell death. In vivo, it can be used by 150 mg/kg/day in mice [3].

References

[1] Ringel F, Kaeda J, Schwarz M, et al. Effects of Jak2 type 1 inhibitors NVP-BSK805 and NVP-BVB808 on Jak2 mutation-positive and Bcr-Abl-positive cell lines. Acta Haematol. 2014, 132(1):75-86.
[2] Baffert F, R?gnier CH, De Pover A, et al. Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805. Mol Cancer Ther. 2010, 9(7):1945-1955.
[3] Rubert J, Qian Z, Andraos R, et al. Bim and Mcl-1 exert key roles in regulating JAK2V617F cell survival. BMC Cancer. 2011, 19(11):24.

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