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Angiogenesis JAK AT9283

AT9283

Catalog No. T3068   CAS 896466-04-9
Synonyms: J-504568
Purity 99.98% Datasheet MSDS

AT9283 is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).

AT9283, CAS 896466-04-9
Pack Size Availability Price/USD Quantity
2 mg In stock 70.00
5 mg In stock 100.00
10 mg In stock 193.00
25 mg In stock 347.00
50 mg In stock 573.00
100 mg In stock 920.00
1 mL * 10 mM (in DMSO) In stock 100.00
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Biological Description
Chemical Properties
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Description AT9283 is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).
Targets&IC50 Abl1 (T315I) :ic50 4nM,   Aurora A :ic50 ~3.0nM,   Aurora B :ic50 ~3.0nM,   JAK2 :ic50 1.2nM,   JAK3 :ic50 1.1nM,  
Kinase Assay Aurora A and Aurora B Kinase Assays: Assays for Aurora A and B are performed in a DELFIA format. Aurora A enzyme is incubated with AT9283 and 3 μM cross-tide substrate (biotin-CGPKGPGRRGRRRTSSFAEG) in 10 mM MOPS, pH 7, 0.1 mg/mL BSA, 0.001% Brij-35, 0.5% glycerol, 0.2 mM EDTA, 10 mM MgCl2, 0.01% β-mercaptoethanol, 15 μM ATP, and 2.5% DMSO. Aurora B enzyme is incubated with AT9283, 3 μM of the above substrate in 25 mM Tris, pH 8.5, 5 mM MgCl2, 0.1 mg/mL BSA, 0.025% Tween-20, 1 mM DTT, 15 μM ATP, and 2.5% DMSO. Reactions are allowed to proceed for 60 minutes and 45-90 minutes for Aurora A and Aurora B, respectively, before quenching with EDTA. The reaction mixtures are then transferred to a neutravidin-coated plate, and phosphorylated peptide is quantified by means of a phospho-specific antibody and a europium labeled secondary antibody using time-resolved fluorescence (excitation, 337 nm; emission, 620 nm). IC50 values for the control compounds are 92 nM (Aurora A assay) and 17 nM (Aurora B).
Cell Research
HCT 116 cells are cultured in DMEM + 10% FBS + GLUTAMAX I. Black 96-well flat-bottomed (clear) tissue culture treated plates are seeded in 200 μL of medium and incubated for approximately 16 hours at 37°C in a humidified atmosphere of 5% CO2 in air. Cells are treated with test compound at nine different concentrations (spanning 1 nM to 10 μM, plus DMSO vehicle control) and then incubated for 72 hours. Polyploidy morphological observations of the cells are then noted. The concentration of AT9283 required to produce a distinct polyploid phenotype is reported. Cells are seeded at a concentration of 75−100 cells/mL relevant culture media onto 6- or 24-well tissue culture plates and allowed to recover for 16 hours. Test compound (11 concentrations spanning 0.1 nM to 10 μM) or vehicle control (DMSO) is added to duplicate wells to give a final DMSO concentration of 0.1%. Following compound addition, colonies are allowed to grow between 10 and 14 days for optimum discrete colony counting. Colonies are fixed in 2 mL of Carnoys fixative (25% acetic acid, 75% MeOH) and stained in 2 mL of 0.4% w/v crystal violet. The numbers of colonies in each well is counted. IC50 values are calculated by sigmoidal dose-response (variable slope) IC50 curves using Prism Graphpad software. (Only for Reference)
Cell lines: HCT 116 cells
Animal Research
Animal Model: HCT116 cells are injected s.c. Into the hind flank of BALB/c mice.
Synonyms J-504568
Purity 98.45%
Molecular Weight 381.43
Formula C19H23N7O2
CAS No. 896466-04-9

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 71 mg/mL (186.1 mM)

Ethanol: 22 mg/mL (57.7 mM)

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

15% Captisol: 10 mg/mL

Citations

References and Literature
1. Howard S, et al. J Med Chem, 2009, 52(2), 379-388. 2. Qi W, et al. Int J Cancer. 2012, 130(12), 21997-32005. 3. Santo L, et al. Clin Cancer Res. 2011, 17(10), 3259-3271.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Stem cell Differentiation Compound Library Autophagy Compound Library Epigenetics Compound Library DNA Damage & Repair Compound Library Cytokine Inhibitor Library Kinase Inhibitor Library Anti-cancer Clinical Compound Library Angiogenesis related Compound Library JAK STAT Compound Library Cell cycle related Compound Library

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