NVP-BSK805 trihydrochloride

Modify Date: 2024-01-10 10:57:56

NVP-BSK805 trihydrochloride structure	Common Name	NVP-BSK805 trihydrochloride
	CAS Number	2320258-95-3	Molecular Weight	599.93
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₇H₃₁Cl₃F₂N₆O	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of NVP-BSK805 trihydrochloride

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].

Name	NVP-BSK805 trihydrochloride

Description	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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> JAK/STAT Signaling >> JAK Signaling Pathways >> Epigenetics >> JAK Signaling Pathways >> Stem Cell/Wnt >> JAK
Target	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)
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 and JAK3 inhibition in the 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].
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].
References	[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.

Molecular Formula	C₂₇H₃₁Cl₃F₂N₆O
Molecular Weight	599.93

NVP-BSK805 trihydrochloride

Use of NVP-BSK805 trihydrochloride

Names

NVP-BSK805 trihydrochloride Biological Activity

Chemical & Physical Properties