[CAS NO. 1942919-79-0] NVP-BSK805dihydrochloride
PRODUCTS SPECIFICATIONS [1942919-79-0]
DESCRIPTION [1942919-79-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 563.47 |
| Molecular Formula | C27H30Cl2F2N6O |
| SMILES | FC1=C(CN2CCOCC2)C(F)=CC(C3=C4N=C(C5=CN(C6CCNCC6)N=C5)C=NC4=CC=C3)=C1.Cl.Cl |
1 Publications Citing Use of MCE
Summary
IC50 & Target
|
JAK2 JH1 0.48 nM (IC 50 ) |
FL JAK2 V617F 0.56 nM (IC 50 ) |
FL JAK2 wt 0.58 nM (IC 50 ) |
TYK2 JH1 10.76 nM (IC 50 ) |
JAK3 JH1 18.68 nM (IC 50 ) |
JAK1 JH1 31.63 nM (IC 50 ) |
In Vitro
NVP-BSK805 dihydrochloride (BSK805 dihydrochloride) is a JAK2 inhibitor, with IC
50
s 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 inhibits the full-length wild-type JAK2 (FL JAK2 wt) and FL JAK2 V617F activity, with IC
50
s of 0.58 ± 0.03 and 0.56 ± 0.04 nM. NVP-BSK805 is ATP-competitive, with aclculated K
i
of 0.43 ± 0.02 nM. NVP-BSK805 suppresses the growth of JAK2
V617F
-bearing acute myeloid leukemia cell lines with GI
50
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 JAK2
V617F
-mutant cell lines
[1]
.
NVP-BSK805 dihydrochloride (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
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
NVP-BSK805 (BSK805 dihydrochloride; 150 mg/kg, p.o.) blocks STAT5 phosphorylation, splenomegaly, and leukemic cell spreading in a Ba/F3 JAK2
V617F
cell-driven mouse model
[1]
.
NVP-BSK805 (50, 75, and 100 mg/kg, p.o.) also suppresses rhEpo-mediated polycythemia and splenomegaly in BALB/c mice
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 50 mg/mL ( 88.74 mM ; Need ultrasonic)
H 2 O : < 0.1 mg/mL (insoluble)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7747 mL | 8.8736 mL | 17.7472 mL |
| 5 mM | 0.3549 mL | 1.7747 mL | 3.5494 mL |
| 10 mM | 0.1775 mL | 0.8874 mL | 1.7747 mL |
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] 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.