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Submit ReviewNVP 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.
NVP BSK 805 is also offered as part of the Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
M. Wt | 599.94 |
Formula | C27H28F2N6O.3HCl |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 2320258-95-3 |
PubChem ID | 131648244 |
InChI Key | VWBSZLCFZWKXHV-UHFFFAOYSA-N |
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 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
Keywords: NVP BSK 805, NVP BSK 805 supplier, NVPBSK805, JAK2, inhibitors, inhibits, potent, orally, bioavailable, AML, acute, myeloid, leukemia, polycythemia, JAK, Kinase, 5818, Tocris Bioscience
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