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AT9283

Cat. No. M1655
AT9283 Structure
Size Price Availability Quantity
5mg USD 140 In stock
10mg USD 210 In stock
50mg USD 620 In stock
100mg USD 1030 In stock
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Quality Control
Biological Activity

AT9283 is a potent inhibitor of several protein kinases, including Aurora A, Aurora B, Janus kinase 2 (JAK2), JAK3, and ABL. AT9283 potently inhibited proliferation and Jak2-related signalling in Jak2-dependent cell lines. The compound also demonstrated significant therapeutic potential in vivo in an ETV6-JAK2 (TEL-JAK2) murine leukaemia model.

Protocol
Cell Experiment
Cell lines HCT 116 cells
Preparation method Primary HCT116 Cellular Assay. HCT 116 cells were cultured in DMEM + 10% FBS + GLUTAMAX I. Black 96-well flat bottomed (clear) tissue culture treated plates were seeded at 5 × 103 cells per well in 200 µL of medium and incubated for approximately 16 h at 37 °C in a humidified atmosphere of 5% CO2 in air. Cells were treated with test compound at nine different concentrations (spanning 1 nM to 10 µM, plus DMSO vehicle control) and then incubated for 72 h. Polyploidy morphological observations of the cells were then noted. The concentration of test compound required to produce a distinct polyploid phenotype was reported.
Concentrations 1 nM to 10 µM
Incubation time 72 h
Animal Experiment
Animal models HCT116 Colon Carcinoma Cell Line Xenograft Model
Formulation 10% DMSO, 20% water, 70% hydroxypropyl--cyclodextrin (25% w/v aq)
Dosages 15 and 20mg/kg twice daily (b.i.d. × 2, q4d) × 5
Administration intraperitoneal
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 381.43
Formula C19H23N7O2
CAS Number 896466-04-9
Purity >99%
Solubility DMSO
Storage at -20°C
References

A phase I dose escalation study of AT9283, a small molecule inhibitor of aurora kinases, in patients with advanced solid malignancies.
Arkenau et al. Ann Oncol. 2012 May;23(5):1307-13. PMID: 22015452.

AT9283, a novel aurora kinase inhibitor, suppresses tumor growth in aggressive B-cell lymphomas.
Qi W et al. Int J Cancer. 2012 Jun 15;130(12):2997-3005. PMID: 21796626.

AT-9283, a small-molecule multi-targeted kinase inhibitor for the potential treatment of cancer.
Kimura S Curr Opin Investig Drugs. 2010 Dec;11(12):1442-9. PMID: 21154126.

AT9283, a potent inhibitor of the Aurora kinases and Jak2, has therapeutic potential in myeloproliferative disorders.
Dawson et al. Br J Haematol. 2010 Jul;150(1):46-57. PMID: 20507304.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AT9283 supplier, Aurora Kinase, inhibitors

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