Discontinued Product

NVP BSK 805 (Cat. No. 5818) has been withdrawn from sale for commercial reasons.
Description: Potent JAK2 inhibitor; orally bioavailable
Chemical Name: 8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline trihydrochloride
Purity: ≥98% (HPLC)
Pathways (1)

Biological Activity for NVP BSK 805

NVP BSK 805 is a potent JAK2 inhibitor (IC50 = 0.48 nM). Exhibits >20-fold selectivity for JAK2 over TYK2, JAK3 and JAK1 (IC50 values are 10.8, 18.7 and 31.6 nM, respectively). Inhibits proliferation and induces apoptosis of JAK2V617F-bearing acute myeloid leukemia cells in vitro and in vivo. Also inhibits erythropoietin-induced polycythemia. Orally bioavailable.

Compound Libraries for NVP BSK 805

NVP BSK 805 is also offered as part of the Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for NVP BSK 805

M. Wt 599.94
Formula C27H28F2N6O.3HCl
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 2320258-95-3
PubChem ID 131648244
Smiles FC1=C(CN2CCOCC2)C(F)=CC(C3=C4C(N=CC(C5=CN(C6CCNCC6)N=C5)=N4)=CC=C3)=C1.Cl.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

References for NVP BSK 805

References are publications that support the biological activity of the product.

Baffert et al (2010) Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805. Mol.Cancer Ther. 9 1945 PMID: 20587663

Pissot-Soldermann et al (2010) Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors. Bioorg.Med.Chem.Lett. 20 2609 PMID: 20231096

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Citations for NVP BSK 805

Citations are publications that use Tocris products.

Currently there are no citations for NVP BSK 805.

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Pathways for NVP BSK 805

JAK-STAT Signaling Pathway

JAK-STAT Signaling Pathway

The JAK-STAT signaling pathway has several roles, including the control of cell proliferation and hematopoiesis. It is the main signal transduction cascade from cytokine receptors.