NVP-BSK805 Chemical Properties

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

NVP-BSK805 Usage And Synthesis

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

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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