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AZ960

Chemical Structure : AZ960

CAS No.: 905586-69-8

AZ960 (AZ-960;AZ 960)

Catalog No.: PC-42571Not For Human Use, Lab Use Only.

A potent, selective JAK2 inhibitor with Ki of 0.45 nM, IC50 of <3 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

A potent, selective JAK2 inhibitor with Ki of 0.45 nM, IC50 of <3 nM; displays 3-fold selectivity over JAK3 (IC50=9 nM); blocks STAT5 phosphorylation and potently inhibits cell proliferation (GI50=25 nM) in TEL-JAK2 driven Ba/F3 cells, blocks BCL-XL, PIM1 and PIM2 mRNA expression and induces apoptosis; also induces growth arrest and apoptosis in adult T-cell leukemia cells; also inhibits parasite Trypanosoma brucei ERK8 (Ki=1.25 uM) with antiparasitic activity (IC50=120nM).

Blood Cancer

Preclinical

Physicochemical Properties

M.Wt 354.3566464
Formula C18H16F2N6
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 30 mg/mL

Chemical Name/SMILES

3-Pyridinecarbonitrile, 5-fluoro-2-[[(1S)-1-(4-fluorophenyl)ethyl]amino]-6-[(5-methyl-1H-pyrazol-3-yl)amino]-

References

1. Gozgit JM, et al. J Biol Chem. 2008 Nov 21;283(47):32334-43.

2. Yang J, et al. Mol Cancer Ther. 2010 Dec;9(12):3386-95.

3. Valenciano AL, et al. Bioorg Med Chem. 2016 Oct 1;24(19):4647-4651.

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