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NVP-BSK805 dihydrochloride

Cat. No. M1804
NVP-BSK805 dihydrochloride Structure
Synonym:

NVP-BSK805, BSK805

Size Price Availability Quantity
10mg USD 200 In stock
50mg USD 750 In stock
100mg USD 1080 In stock
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Quality Control
Biological Activity

NVP-BSK805 dihydrochloride is a potent and selective quinoxaline JAK2 inhibitor with IC50 values of 0.48, 0.56 and 0.58 nM for JAK2 JH1, FL JAK V617F and FL JAK2 wt respectively. Within the JAK family, NVP-BSK805 displays more than 20-fold selectivity towards JAK2 in vitro, as well as excellent selectivity in broader kinase profiling. The compound blunts constitutive STAT5 phosphorylation in JAK2(V617F)-bearing cells, with concomitant suppression of cell proliferation and induction of apoptosis. In vivo, NVP-BSK805 exhibited good oral bioavailability and a long half-life. The inhibitor was efficacious in suppressing leukemic cell spreading and splenomegaly in a Ba/F3 JAK2(V617F) cell-driven mouse mechanistic model. Furthermore, NVP-BSK805 potently suppressed recombinant human erythropoietin-induced polycythemia and extramedullary erythropoiesis in mice and rats.

Customer Product Validations & Biological Datas
Source Acta Haematol (2014). Figure 4. NVP-BSK805
Method Western blot
Cell Lines SET-2 and HEL cell line
Concentrations 0.01, 0.05, 0.1, 0.5, 1.0 μM
Incubation Time 24 h
Results The JAK2-positive cell line SET-2 showed suppression of STAT5a phosphorylation already at a concentration of 0.1 μ M of NVP-BSK805 and NVP-BVB808, whereas in HEL cells higher concentrations
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 563.47
Formula C27H28F2N6O.2HCl
CAS Number 1092499-93-8
Purity >99%
Solubility DMSO
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: NVP-BSK805 dihydrochloride, NVP-BSK805, BSK805 supplier, JAK, inhibitors

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