| Identification | Back Directory | [Name]
NVP-BSK805 | [CAS]
1092499-93-8 | [Synonyms]
BSK805
CS-550
CS-1571
BSK-805
BSK 805
NVP-BSK805
NVP-GSK 805
NVP-BSK805 2HCl
NVP-BSK805 - BSK 805
NVP-BSK805 USP/EP/BP
NVP-BSK805(freebase)
NVP-BSK805 dihydrochloride
BSK 805; BSK-805; BSK805; NVP-BSK 805
4-(2,6-Difluoro-4-(3-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)quinoxalin-5-yl)benzyl)morpholine
8-(3,5-difluoro-4-(morpholinomethyl)phenyl)-2-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)quinoxaline
8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline
Quinoxaline, 8-[3,5-difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]- | [Molecular Formula]
C27H28F2N6O | [MDL Number]
MFCD22420810 | [MOL File]
1092499-93-8.mol | [Molecular Weight]
490.55 |
| Chemical Properties | Back Directory | [Melting point ]
137℃ | [Boiling point ]
639.8±55.0 °C(Predicted) | [density ]
1.4 | [storage temp. ]
Store at -20°C | [solubility ]
≥20.95 mg/mL in DMSO; ≥3.45 mg/mL in H2O with gentle warming and ultrasonic; ≥4.75 mg/mL in EtOH with gentle warming and ultrasonic | [form ]
solid | [pka]
9.78±0.10(Predicted) | [color ]
Off-white to yellow |
| Hazard Information | Back Directory | [Uses]
NVP-BSK805 is an ATP-competitive JAK2 inhibitor, with IC50s 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[1]. | [in vivo]
NVP-BSK805 (BSK 805; 150 mg/kg, p.o.) blocks STAT5 phosphorylation, splenomegaly, and leukemic cell spreading in a Ba/F3 JAK2V617F 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].
| [target]
JAK2 | [IC 50]
JAK2 JH1: 0.48 nM (IC50); FL JAK2 V617F: 0.56 nM (IC50); FL JAK2 wt: 0.58 nM (IC50); TYK2 JH1: 10.76 nM (IC50); JAK3 JH1: 18.68 nM (IC50); JAK1 JH1: 31.63 nM (IC50) | [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. DOI:10.1158/1535-7163.MCT-10-0053
[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. DOI:10.1016/j.bbrc.2017.06.178 |
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