NVP BSK 805

Pricing Availability Delivery Time Qty
Cat.No. 5818 - NVP BSK 805 | C27H28F2N6O.3HCl
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)
Datasheet
Citations
Reviews
Literature
Pathways

Biological Activity

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.

Technical Data

M. Wt 599.94
Formula C27H28F2N6O.3HCl
Storage Store at +4°C
Purity ≥98% (HPLC)
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 30 50
water 59.99 100

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 solvent 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

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

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Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

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  • Cell Cycle and DNA Damage Repair
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  • Invasion and Metastasis
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  • Complement System
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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

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Pathways for NVP BSK 805

JAK-STAT

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.