NVP-BSK805 dihydrochloride 是一种有效的选择性 JAK2 抑制剂，对 JAK2、TYK2、JAK3 和 JAK1 的 IC50 分别为 0.5 nM、10.76 nM、18.68 nM 和 31.63 nM。

NVP-BSK805 dihydrochloride is an effective and selective inhibitor of JAK2 with IC50s of 0.5 nM, 10.76 nM, 18.68 nM, and 31.63 nM for JAK2, TYK2, JAK3, and JAK1.

In JAK2V617F-mutated cells, NVP-BSK805 dihydrochloride (100 nM) significantly inhibits the phosphorylation of STAT5 like MB-02. Incubation of SET-2 cells with NVP-BSK805 dihydrochloride (150 nM and 1 μM) inhibits cell growth in a concentration- and time-dependent manner by 75% and 95%, respectively[1]. In JAK2 (V617F), SET-2, and MB-02 cells, NVP-BSK805 dihydrochloride regulates the post-translational modification of Bim and the level of Mcl-1[2].

The utilization efficiency of oral NVP-BSK805 dihydrochloride biopharmaceuticals was estimated to be 45% in mice and 50% in rats. Oral administration of 150 mg/kg NVP-BSK805 dihydrochloride to a mouse model harboring Ba/F3 JAK2V617F cells inhibited STAT5 phosphorylation, splenomegaly, and leukemia cell proliferation. Oral administration of 25, 50 and 100 mg/kg of NVP-BSK805 dihydrochloride to BALB/c mice inhibited rhEpo-induced STAT5 phosphorylation and rhEpo-regulated erythrocytosis and splenomegaly[1].

Cells can be detected by colorimetric assay kit WST-1 (Roche Diagnostics GmbH) The survival rate was used to analyze and compare the survival of cells after 72 hours of incubation with 8-point concentration range of drugs and the related changes in cell proliferation after treatment of cells with DMSO, which can detect the ability of JAK2 inhibitors to inhibit cell proliferation. After three repetitions, the mean value was calculated and plotted with XLfit 4 software to obtain the value of half of the maximum growth inhibition (GI50).

1942919-79-0

C27H30Cl2F2N6O

563.47

盐酸NVP-BSK805;BSK 805;NVP-BSK805 (dihydrochloride)

DMSO:40 mg/mL (71 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years