Powder: -20°C for 3 years
In solvent: -80°C for 2 years
NVP-BSK805 is an ATP-competitive JAK2 inhibitor.
Description | NVP-BSK805 is an ATP-competitive JAK2 inhibitor. |
Targets&IC50 | JAK1 JH1:31.63 nM, FL JAK2 V617F:0.56 nM, TYK2 JH1:10.76 nM, JAK3 JH1:18.68 nM, JAK2 JH1:0.48 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. |
Synonyms | BSK 805, NVP-BSK805 2HCl |
Molecular Weight | 490.54 |
Formula | C27H28F2N6O |
CAS No. | 1092499-93-8 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 10mM
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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NVP-BSK805 1092499-93-8 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors Tyrosine Kinases JAK Inhibitor ATP-competitive NVP-BSK-805 Janus kinase NVP BSK805 JAK1 inhibit NVPBSK805 BSK 805 homology TYK2 JAK3 NVP-BSK805 2HCl JH1 JAK2 inhibitor