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NVP-BSK805

Catalog No. T5049 CAS 1092499-93-8

Synonyms: NVP-BSK805 2HCl, BSK 805

NVP-BSK805 (BSK 805) is an ATP-competitive JAK2 inhibitor.

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NVP-BSK805, CAS 1092499-93-8

Pack Size	Availability	Price/USD
1 mg	5 days	$ 57.00
5 mg	5 days	$ 133.00
10 mg	5 days	$ 220.00
25 mg	5 days	$ 432.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	NVP-BSK805 (BSK 805) is an ATP-competitive JAK2 inhibitor.
Targets&IC50	FL JAK2 (WT):0.58 nM, JAK2 JH1:0.48 nM, JAK3 JH1:18.68 nM, TYK2 JH1:10.76 nM, FL JAK2 (V617F):0.56 nM, JAK1 JH1:31.63 nM
In vitro	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 JAK2V617F-mutant cell lines. NVP-BSK805 (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 (150 mg/kg, p.o.) blocks STAT5 phosphorylation, splenomegaly, and leukemic cell spreading in a Ba/F3 JAK2V617F 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.

Synonyms	NVP-BSK805 2HCl, BSK 805
Molecular Weight	490.55
Formula	C27H28F2N6O
CAS No.	1092499-93-8

Storage

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

Solubility Information

DMSO: 10mM

References and Literature

1. 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. 2. Rubert J, et al. BMC Cancer, 2011, Jan(19), 11-24. 3. 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.

Related compound libraries

This product is contained In the following compound libraries：

Fluorochemical Library Tyrosine Kinase Inhibitor Library NO PAINS Compound Library

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Related compounds with same targets

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

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

NVP-BSK805 1092499-93-8 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors Tyrosine Kinases JAK Inhibitor ATP-competitive Janus kinase BSK805 NVP BSK805 JAK1 inhibit NVP-BSK805 2HCl NVP-BSK 805 NVPBSK805 homology TYK2 JAK3 NVP-BSK-805 BSK-805 JH1 BSK 805 JAK2 inhibitor

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