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NVP-BSK805 dihydrochloride

CAS No. : 1942919-79-0

MCE 站：NVP-BSK805 dihydrochloride

产品活性：NVP-BSK805 dihydrochloride 是一种 ATP 竞争性的 JAK2 抑制剂，对 JAK2 JH1 (JAK 同源 1)，JAK1 JH1，JAK3 JH1，和 TYK2 JH1 的 IC₅₀ 值分别为 0.48 nM，31.63 nM，18.68 nM 和 10.76 nM。

研究领域：Epigenetics  |  Stem Cell/Wnt  |  JAK/STAT Signaling

作用靶点：JAK

In Vitro: NVP-BSK805 dihydrochloride (BSK805 dihydrochloride) is a JAK2 inhibitor, with IC₅₀s of 0.48 nM, 31.63 nM, 18.68 nM, ａnd 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, ａnd TYK2 JH1, respectively. NVP-BSK805 inhibits the full-length wild-type JAK2 (FL JAK2 wt) ａnd FL JAK2 V617F activity, with IC₅₀s of 0.58 ± 0.03 ａnd 0.56 ± 0.04 nM. NVP-BSK805 is ATP-competitive, with aclculated K_i of 0.43 ± 0.02 nM. NVP-BSK805 suppresses the growth of JAK2^V617F-bearing acute myeloid leukemia cell lines with GI₅₀ of <100 nM. NVP-BSK805 blocks the STAT5 phosphorylation at ≥100 nM concentrations, ａnd shows a bias for JAK2 over JAK1 ａnd JAK3 inhibition in the JAK2^V617F-mutant cell lines.
NVP-BSK805 dihydrochloride (5 μM) improves P-gp inhibitory activity. NVP-BSK805 increases sensitization of drug-resistant KBV20C cancer cells to VIC treatment at 10 μM, ａnd such an effect is more effective than a 5 μM dose.

In Vivo: NVP-BSK805 (BSK805 dihydrochloride; 150 mg/kg, p.o.) blocks STAT5 phosphorylation, splenomegaly, ａnd leukemic cell spreading in a Ba/F3 JAK2^V617F cell-driven mouse model.
NVP-BSK805 (50, 75, ａnd 100 mg/kg, p.o.) also suppresses rhEpo-mediated polycythemia ａnd splenomegaly in BALB/c mice.

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