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AT-9283 L-lactate

Names

[ CAS No. ]:
896466-76-5

[ Name ]:
AT-9283 L-lactate

[Synonym ]:
1-Cyclopropyl-3-{3-[5-(morpholin-4-ylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl}harnstoff
1-Cyclopropyl-3-{3-[5-(4-morpholinylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl}urea
1-cyclopropyl-3-{3-[5-(morpholin-4-ylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl}urea
Urea, N-cyclopropyl-N'-[3-[5-(4-morpholinylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl]-

Biological Activity

[Description]:

AT9283 lactic acid is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 lactic acid inhibits growth and survival of multiple solid tumors in vitro and in vivo[1][2].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> Aurora Kinase
Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> Aurora Kinase
Signaling Pathways >> JAK/STAT Signaling >> JAK
Signaling Pathways >> Epigenetics >> JAK
Signaling Pathways >> Stem Cell/Wnt >> JAK
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Bcr-Abl
Signaling Pathways >> Autophagy >> Autophagy
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FLT3

[Target]

Aurora A:3 nM (IC50)

Aurora B:3 nM (IC50)

JAK3:1.1 nM ()

JAK2:1.2 nM ()

ABL(T315I):4 nM ()


[References]

[1]. Howard S, et al. Fragment-Based Discovery of the Pyrazol-4-yl Urea (AT9283), a Multitargeted Kinase Inhibitor with Potent Aurora Kinase Activity. Journal of Medicinal Chemistry (2009), 52(2), 379-388.  

[2]. Qi W, et al. AT9283, a novel aurora kinase inhibitor, suppresses tumor growth in aggressive B-cell lymphomas. Int J Cancer. 2012 Jun 15;130(12):2997-3005.  

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C22H29N7O5

[ Molecular Weight ]:
471.51

[ Exact Mass ]:
381.191315

[ LogP ]:
0.92

[ Index of Refraction ]:
1.715

Related Compounds