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AT9283
Catalog No.S1134
For research use only.
AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl1(T315I). Phase 2.
CAS No. 896466-04-9
Selleck's AT9283 has been cited by 23 publications
Purity & Quality Control
Choose Selective JAK Inhibitors
Related Compound Libraries
Other JAK Products
Biological Activity
| Description | AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl1(T315I). Phase 2. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Targets |
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| In vitro |
AT9283 leads to a clear polyploid phenotype by inhibiting the activity of Aurora B kinase in HCT116 cells with IC50 of 30 nM. Furthermore, AT9283 also produces the potent inhibition on HCT116 colony formation. [1] |
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| Cell Data |
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| Assay |
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| In vivo | In HCT116 human colon carcinoma xenograft bearing mice, AT9283 treatment (15 mg/kg and 20 mg/kg) for 16 days results in a significant tumor growth inhibition of 67% and 76%, respectively. In addition, AT9283 also exhibits a significantly longer half-life in tumors(2.5 hours) compared with plasma (0.5 hour) and modest oral bioavailability in mice (Fp.o. = 24%). [1] |
Protocol (from reference)
| Kinase Assay: |
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| Cell Research: |
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| Animal Research: |
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| References |
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Solubility (25°C)
|
In vitro |
DMSO |
76 mg/mL
(199.25 mM) |
| Ethanol |
38 mg/mL
(99.62 mM) |
|
| Water |
Insoluble
|
|
|
In vivo |
Add solvents to the product individually and in order |
5mg/mL |
Chemical Information
| Molecular Weight | 381.43 | ||
|---|---|---|---|
| Formula | C19H23N7O2 |
||
| CAS No. | 896466-04-9 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | C1CC1NC(=O)NC2=C(NN=C2)C3=NC4=C(N3)C=C(C=C4)CN5CCOCC5 | ||
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
mg/kg
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.
Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT01145989 | Completed | Drug: AT9283 | Multiple Myeloma | NCIC Clinical Trials Group|Astex Pharmaceuticals Inc.|Canadian Cancer Trials Group | June 15 2010 | Phase 2 |
| NCT00443976 | Completed | Drug: Aurora kinase inhibitor AT9283 | Non-Hodgkins Lymphoma|Unspecified Adult Solid Tumor Protocol Specific | NCIC Clinical Trials Group|Astex Pharmaceuticals Inc.|Canadian Cancer Trials Group | January 4 2007 | Phase 1 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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