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NVP BSK 805
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.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 599.94. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.67 mL||8.33 mL||16.67 mL|
|5 mM||0.33 mL||1.67 mL||3.33 mL|
|10 mM||0.17 mL||0.83 mL||1.67 mL|
|50 mM||0.03 mL||0.17 mL||0.33 mL|
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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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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