AT9283 - CAS 896466-04-9
Catalog number: B0084-100114
Category: Inhibitor
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Molecular Formula:
C19H23N7O2
Molecular Weight:
381.43
COA:
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Targets:
Aurora Kinase
Description:
AT-9283 is a broad spectrum kinase inhibitor that potently inhibits Aurora A, Aurora B, JAK2, JAK3, and c-ABL (IC50= 3, 3, 1.2, 1.1, and 4 nM, respectively). It also potently (IC50 = <1 μM) inhibits serine/threonine kinases as well as receptor and non-receptor tyrosine kinases.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-100114 10 mg $189 In stock
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Purity:
>98%
Synonyms:
AT9283; AT 9283; AT-9283
MSDS:
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InChIKey:
VRXXZJLHPWWXIX-ZCXUNETKSA-N
InChI:
InChI=1S/C19H23N7O2/c27-19(21-13-2-3-13)24-16-10-20-25-17(16)18-22-14-4-1-12(9-15(14)23-18)11-26-5-7-28-8-6-26/h1,4,9-10,13,20,25H,2-3,5-8,11H2,(H2,21,24,27)/b18-17-
Canonical SMILES:
C1CC1NC(=O)NC2=CNNC2=C3N=C4C=CC(=CC4=N3)CN5CCOCC5
1.A phase I trial of AT9283 (a selective inhibitor of aurora kinases) in children and adolescents with solid tumors: a Cancer Research UK study.
Moreno L1, Marshall LV2, Pearson AD2, Morland B3, Elliott M4, Campbell-Hewson Q5, Makin G6, Halford SE7, Acton G7, Ross P7, Kazmi-Stokes S7, Lock V8, Rodriguez A8, Lyons JF8, Boddy AV9, Griffin MJ9, Yule M8, Hargrave D10. Clin Cancer Res. 2015 Jan 15;21(2):267-73. doi: 10.1158/1078-0432.CCR-14-1592. Epub 2014 Nov 4.
PURPOSE: A phase I trial of AT9283 (a multitargeted inhibitor of Aurora kinases A and B) was conducted in children and adolescents with solid tumors, to identify maximum-tolerated dose (MTD), safety, efficacy, pharmacokinetics, and pharmacodynamic (PD) activity.
2.NCIC CTG IND.181: phase I study of AT9283 given as a weekly 24 hour infusion in advanced malignancies.
Dent SF1, Gelmon KA, Chi KN, Jonker DJ, Wainman N, Capier CA, Chen EX, Lyons JF, Seymour L. Invest New Drugs. 2013 Dec;31(6):1522-9. doi: 10.1007/s10637-013-0018-9. Epub 2013 Sep 27.
PURPOSE: AT9283 is a potent inhibitor of the mitotic regulators, Aurora-kinases A and B, and has shown anti-tumor activity in patients with solid and haematological malignancies. This phase I study assessed safety, tolerability, pharmacokinetic and pharmacodynamic properties of AT9283.
3.Strategies to circumvent the T315I gatekeeper mutation in the Bcr-Abl tyrosine kinase.
Bose P1, Park H, Al-Khafaji J, Grant S. Leuk Res Rep. 2013 Jan 1;2(1):18-20.
Despite the remarkable success of imatinib against Bcr-Abl, development of secondary resistance, most often due to point mutations in the Bcr-Abl tyrosine kinase (TK) domain, is quite common. Of these, the T315I "gatekeeper" mutation is resistant to all currently registered Bcr-Abl TK inhibitors (TKIs) with the notable exception of ponatinib (Iclusig™), which was very recently approved by the United States Food and Drug Administration (FDA). Besides ponatinib, numerous strategies have been developed to circumvent this problem. These include the protein synthesis inhibitor omacetaxine (Synribo®), and "switch-control" inhibitors. Dual Bcr-Abl and aurora kinase inhibitors represent another promising strategy. Finally, several promising synergistic combinations, such as TKIs with histone deacetylase inhibitors (HDACIs), warrant attention.
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CAS 896466-04-9 AT9283

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