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AZ 960JAKs inhibitor

AZ 960

Catalog No. A4144
Size Price Stock Qty
2mg $150.00 In stock
5mg $260.00 In stock
10mg $410.00 In stock
50mg $990.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Quality Control & MSDS

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Chemical structure

AZ 960

Biological Activity

Description AZ 960 is a potent, selective and ATP competitive inhibitor of JAK2 with Ki value of 0.45 nM.
Targets JAK2          
IC50 0.45 nM (Ki)          

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Chemical Properties

Cas No. 905586-69-8 SDF Download SDF
Synonyms AZ-960,AZ960
Chemical Name 5-fluoro-2-[[(1S)-1-(4-fluorophenyl)ethyl]amino]-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyridine-3-carbonitrile
Canonical SMILES CC1=CC(=NN1)NC2=C(C=C(C(=N2)NC(C)C3=CC=C(C=C3)F)C#N)F
Formula C18H16F2N6 M.Wt 354.36
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

AZ960 is a novel inhibitor of janus-associated kinases (JAKs) that exhibits a potent inhibition against janus kinase 2 (JAK2) with the value of inhibition constant of Ki of 0.45 nmol/L. It also exhibits a lesser inhibitory effects against other JAKs family members, including JAK1, JAK3 and TYK2 as well as other kinases, including TrkA, Aurora A and FAK, with 50% inhibition concentration IC50 of around 0.1 μmol/L. In recent studies, AZ960 demonstrates potential anti-cancer activity against adult T-cell leukemia (ATL), an aggressive malignancy of CD4+ T lymphocytes, by effectively inducing growth arrest and apoptosis in human T-cell lumphotropic virus type 1 (HTLV-1) infected T cells.

Reference

Yang J, Ikezoe T, Nishioka C, Furihata M, Yokoyama A. AZ960, a novel Jak2 inhibitor, induces growth arrest and apoptosis in adult T-cell leukemia cells. Mol Cancer Ther. 2010;9(12):3386-3395.