NVP-BSK805 trihydrochloride

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

NVP-BSK805 trihydrochloride 

NVP-BSK805 trihydrochloride 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。

NVP-BSK805 trihydrochloride

NVP-BSK805 trihydrochloride Chemical Structure

CAS No. : 2320258-95-3

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NVP-BSK805 trihydrochloride 的其他形式现货产品:

NVP-BSK805 dihydrochloride

生物活性

NVP-BSK805 trihydrochloride trihydrochloride is an ATP-competitive 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[1].

IC50 & Target[1]

JAK2 JH1

0.48 nM (IC50)

JAK2(V617F)

0.56 nM (IC50)

FL JAK2 wt

0.58 nM (IC50)

TYK2 JH1

18.68 nM (IC50)

JAK1 JH1

31.68 nM (IC50)

体外研究
(In Vitro)

NVP-BSK805 trihydrochloride (BSK 805) 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 trihydrochloride 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 trihydrochloride is ATP-competitive, with aclculated Ki of 0.43 ± 0.02 nM. NVP-BSK805 trihydrochloride suppresses the growth of JAK2V617F-bearing acute myeloid leukemia cell lines with GI50 of <100 nm. nvp-bsk805 trihydrochloride blocks the stat5 phosphorylation at ≥100 nm concentrations, and shows a bias for jak2 over jak1 jak3 inhibition in jak2V617F-mutant cell lines[1].
NVP-BSK805 trihydrochloride (5 μM) improves P-gp inhibitory activity. NVP-BSK805 trihydrochloride 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[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

NVP-BSK805 trihydrochloride (BSK 805; 150 mg/kg, p.o.) blocks STAT5 phosphorylation, splenomegaly, and leukemic cell spreading in a Ba/F3 JAK2V617F cell-driven mouse model[1].
NVP-BSK805 trihydrochloride (50, 75, and 100 mg/kg, p.o.) also suppresses rhEpo-mediated polycythemia and splenomegaly in BALB/c mice[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

599.93

Formula

C27H31Cl3F2N6O
CAS 号

2320258-95-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Baffert F, et al. Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805. Mol Cancer Ther. 2010 Jul;9(7):1945-55.

    [2]. [2].Cheon JH, et al. The JAK2 inhibitors CEP-33779 and NVP-BSK805 have high P-gp inhibitory activity and sensitize drug-resistant cancer cells to vincristine. Biochem Biophys Res Commun. 2017 Sep 2;490(4):1176-1182.

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