AT9283 - CAS 896466-04-9
Catalog number: B0084-100114
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C19H23N7O2
Molecular Weight:
381.43
COA:
Inquire
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
Bulk Inquiry
Publictions citing BOC Sciences Products
  • >> More
Purity:
>98%
MSDS:
Inquire
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.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Aurora Kinase Products


CAS 639089-54-6 Tozasertib

Tozasertib
(CAS: 639089-54-6)

The Aurora kinases (A, B, and C) are a family of serine-threonine kinases that regulate various stages of mitotic function. With significant roles in cell cycle...

CAS 885325-71-3 MK-8745

MK-8745
(CAS: 885325-71-3)

MK-8745 is a novel Aurora-A specific inhibitor. MK8745 induced apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lin...

CAS 934541-31-8 TAK-901

TAK-901
(CAS: 934541-31-8)

TAK-901 is a small-molecule inhibitor of the serine-threonine kinase Aurora B with potential antineoplastic activity. Aurora B kinase inhibitor TAK-901 binds to...

CAS 1095382-05-0 CCT-137690

CCT-137690
(CAS: 1095382-05-0)

CCT137690, an aurora kinase inhibitor CCT137690, is a highly selective, orally bioavailable imidazo[4,5-b]pyridine derivative that inhibits Aurora A and B kinas...

CAS 934353-76-1 ENMD-2076

ENMD-2076
(CAS: 934353-76-1)

ENMD-2076 is an orally-active, Aurora A/angiogenic kinase inhibitor with a unique kinase selectivity profile and multiple mechanisms of action. ENMD-2076 has be...

CAS 942918-07-2 GSK-1070916A

GSK-1070916A
(CAS: 942918-07-2)

GSK-1070916A is an ATP-competitive inhibitor of the serine/threonine kinases Aurora B and C with potential antineoplastic activity. Aurora B/C kinase inhibitor ...

CAS 1010085-13-8 MK-5198

MK-5198
(CAS: 1010085-13-8)

MK-5108 is a novel small molecule with potent inhibitory activity against Aurora-A kinase. Although most of the Aurora-kinase inhibitors target both Aurora-A an...

CAS 398493-79-3 PHA-680632

PHA-680632
(CAS: 398493-79-3)

PHA-680632 is a is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM. PHA-680632 is also the first representative of a ...

CAS 896466-04-9 AT9283

AT9283
(CAS: 896466-04-9)

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...

CAS 1291074-87-7 ENMD-2076 L-(+)-Tartaric acid

ENMD-2076 L-(+)-Tartaric acid
(CAS: 1291074-87-7)

ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more selec...

CAS 827318-97-8 Danusertib

Danusertib
(CAS: 827318-97-8)

Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Aurora kinase inhibitor PHA-739358 binds to and inhibits the A...

CAS 1158838-43-7 Aurora A inhibitor II

Aurora A inhibitor II
(CAS: 1158838-43-7)

Aurora A inhibitor II is a potent and selective inhibitor of Aurora A kinase (AurA; IC50 = 4.3 nM).

CAS 1094069-99-4 SCH-1473759

SCH-1473759
(CAS: 1094069-99-4)

SCH-1473759 is a novel sub-nanomolar Aurora A/B inhibitor. SCH 1473759 was active against a large panel of tumor cell lines from different tissue origin and gen...

CAS 1146618-41-8 SNS-314 Mesylate

SNS-314 Mesylate
(CAS: 1146618-41-8)

SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively. It is less potent to T...

CAS 331771-20-1 ZM447439

ZM447439
(CAS: 331771-20-1)

ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM, 130 nM respectively, > 8 fold selectivity than Aurora C

CAS 443797-96-4 JNJ-7706621

JNJ-7706621
(CAS: 443797-96-4)

JNJ-7706621 is a novel cell cycle inhibitor that showed potent inhibition of several cyclin-dependent kinases (CDK) and Aurora kinases and selectively blocked p...

CAS 722544-51-6 AZD-1152HQPA

AZD-1152HQPA
(CAS: 722544-51-6)

AZD-1152HQPA is an active metabolite of Barasertib (AZD-1152), which is a novel acetanilide-substituted pyrazole-aminoquinazoline prodrug that is converted rap...

CAS 422513-13-1 Hesperadin

Hesperadin
(CAS: 422513-13-1)

Hesperadin is  an inhibitor of human Aurora B, which can prevent the phosphorylation of substrate with IC(50) of 40 nM. Growth of cultured bloodstream forms was...

CAS 869363-13-3 MLN8054

MLN8054
(CAS: 869363-13-3)

MLN8054 is an aurora kinase inhibitor MLN8054, which is an orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase...

CAS 945595-80-2 AMG-900

AMG-900
(CAS: 945595-80-2)

AMG 900 is a small-molecule inhibitor of Aurora kinases A, B and C with potential antineoplastic activity. Aurora kinase inhibitor AMG 900 selectively binds to ...

Chemical Structure

CAS 896466-04-9 AT9283

Quick Inquiry

Verification code

Featured Items