A potent, selective JAK2 inhibitor
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NVP-BSK805 (hydrochloride)

Item No. 16714

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(2,6-difluoro-4-(3-(1-(pip4-(2,6-difluoro-4-(3-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)quinoxalin-5-yl)benzyl)morpholine, dihydrochloride
CAS Number
1942919-79-0
Molecular Formula
C27H28F2N6O • 2HCl
Formula Weight
563.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 25 mg/mlEthanol: 1 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
244, 275, 350 nm
SMILES
FC1=C(CN2CCOCC2)C(F)=CC(C3=CC=CC4=C3N=C(C5=CN(C6CCNCC6)N=C5)C=N4)=C1.Cl.Cl
InChi Code
InChI=1S/C27H28F2N6O.2ClH/c28-23-12-18(13-24(29)22(23)17-34-8-10-36-11-9-34)21-2-1-3-25-27(21)33-26(15-31-25)19-14-32-35(16-19)20-4-6-30-7-5-20;;/h1-3,12-16,20,30H,4-11,17H2;2*1H
InChi Key
NUOCAPALWRHKCU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $75

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    5 mg

    $315

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    10 mg

    $442

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    Product Description

    NVP-BSK805 is a potent inhibitor of JAK2 that also inhibits the JAK2V617F mutant enzyme (IC50s for both enzymes ~ 0.5 nM). It displays at least 20-fold selectivity against other JAK enzymes and a panel of serine/threonine and tyrosine kinases.1 This ATP-competitive inhibitor is orally bioavailable and has a long half-life in vivo, suppressing leukemic cell spreading and splenomegaly in JAK2V617F cell-driven disease in mice.1 NVP-BSK805 suppresses recombinant human erythropoietin-induced polycythemia and extramedullary erythropoiesis in mice and rats.1 NVP-BSK805 can be used to study the molecular mechanisms involved in JAK2V617F signaling in cells.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Baffert, F., Régnier, C.H., De Pover, A., et al. Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805. Mol. Cancer Ther. 9(7), 1945-1955 (2010).

    2. Rubert, J., Qian, Z., Andraos, R., et al. Bim and Mcl-1 exert key roles in regulating JAK2V617F cell survival. BMC Cancer 11:24, (2011).