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NVP-BSK805 trihydrochloride

Catalog No. T39858 CAS 2320258-95-3

Synonyms: NVP-BSK805 trihydrochloride

NVP-BSK805 trihydrochloride is a potent ATP-competitive inhibitor of JAK2, exhibiting IC50 values of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM against JAK2 JH1, JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.

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NVP-BSK805 trihydrochloride Chemical Structure

NVP-BSK805 trihydrochloride, CAS 2320258-95-3

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Description	NVP-BSK805 trihydrochloride is a potent ATP-competitive inhibitor of JAK2, exhibiting IC50 values of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM against JAK2 JH1, JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.
Targets&IC50	FL JAK2 (WT):0.58 nM (IC50), JAK2 JH1:0.48 nM (IC50), TYK2 JH1:18.68 nM (IC50), JAK1 JH1:31.68 nM (IC50), JAK2 (V617F):0.56 nM (IC50)
In vitro	NVP-BSK805 trihydrochloride (BSK 805) effectively inhibits JAK2, exhibiting specificity in JAK inhibition with IC50s of 0.48 nM for JAK2 JH1, alongside notable activity against JAK1, JAK3, and TYK2. The compound also targets both the wild-type and V617F mutant forms of full-length JAK2, with IC50s around 0.57 nM, demonstrating its ATP-competitive nature with a Ki of 0.43 nM. Particularly potent against acute myeloid leukemia cells carrying the JAK2 V617F mutation, it achieves significant growth suppression at concentrations below 100 nM and obstructs STAT5 phosphorylation at concentrations of 100 nM or higher, indicating a preference for JAK2 inhibition. Additionally, at a concentration of 5 μM, it enhances P-gp inhibitory activity and at 10 μM, increases the sensitivity of drug-resistant KBV20C cancer cells to VIC treatment, outperforming lower doses in efficacy.
In vivo	NVP-BSK805 trihydrochloride (BSK 805; 150 mg/kg, p.o.) effectively inhibits STAT5 phosphorylation, reduces splenomegaly, and prevents the dissemination of leukemic cells in a Ba/F3 JAK2 V617F cell-driven mouse model[1]. Lower doses of NVP-BSK805 trihydrochloride (50, 75, and 100 mg/kg, p.o.) have also been shown to diminish rhEpo-induced polycythemia and splenomegaly in BALB/c mice[1].

Synonyms	NVP-BSK805 trihydrochloride
Molecular Weight	599.93
Formula	C27H31Cl3F2N6O
CAS No.	2320258-95-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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. 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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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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