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NVP-BSK805 (BSK 805) is an ATP-competitive JAK2 inhibitor.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $57 | 7-10 days | |
5 mg | $133 | 7-10 days | |
10 mg | $220 | 7-10 days | |
25 mg | $432 | 7-10 days |
Description | NVP-BSK805 (BSK 805) is an ATP-competitive JAK2 inhibitor. |
Targets&IC50 | JAK1 JH1:31.63 nM, FL JAK2 (V617F):0.56 nM, TYK2 JH1:10.76 nM, JAK2 JH1:0.48 nM, JAK3 JH1:18.68 nM, FL JAK2 (WT):0.58 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. |
Alias | 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 | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 10 mM | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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