AT9283

For research use only.

Catalog No.S1134

19 publications

AT9283 Chemical Structure

CAS No. 896466-04-9

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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Selleck's AT9283 has been cited by 19 publications

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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.
Targets
JAK3 [1]
(Cell-free assay)		 JAK2 [1]
(Cell-free assay)		 Aurora A [1]
(Cell-free assay)		 Aurora B [1]
(Cell-free assay)		 Abl1 (T315I) [1]
(Cell-free assay)
1.1 nM 1.2 nM ~3.0 nM ~3.0 nM 4 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 cells M1H3ZmN6fG:2b4jpZ:Kh[XO|YYm= M361R|ExNTF2IHThfZM> MYfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO|ZYPz[YQh[XNiboXtZoVzKG:oIHPvcI9vcWW|IHHmeIVzKDFyIITvJFE1KGSjeYOgZpkh[2:ub375JIZwem2rbnegZZN{[XluIFnDOVA:OC5yMUKg{txO MXexPVE1OzV4Nx?=
HT-29 cells M3zNXGZ2dmO2aX;uJIF{e2G7 NE\nT3g4OiCq M4TpZ2FvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUMVI6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6zPFMh|ryP M{nYNFI{PjZ2MEm5
A549 cells NITZ[2NHfW6ldHnvckBie3OjeR?= NUH3TnFYPzJiaB?= MkHWRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwNUGyJO69VQ>? MkfuNlM3PjRyOUm=
LoVo cells Mm\TSpVv[3Srb36gZZN{[Xl? MWO3NkBp MonRRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTH;Wc{Bk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwNUWzJO69VQ>? MoP2NlM3PjRyOUm=
K562 cells NFHhUIFHfW6ldHnvckBie3OjeR?= NXXXVo5uPzJiaB?= NXHufGpGSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gT|U3OiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGuOkDPxE1? M1XrclI{PjZ2MEm5
U937 cells MXLGeY5kfGmxbjDhd5NigQ>? NIPUZoM4OiCq NU\WcIhPSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gWVk{PyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5 MYSyN|Y3PDB7OR?=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 21430070     


AT9283 reduces MM cells viability in a dose dependent manner. Cells were treated with increasing doses of AT9283 for 72 hours and cell viability was measured by MTT assay

21430070
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

Kinase Assay:

[1]
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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:

[1]
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  • Cell lines: HCT 116 cells
  • Concentrations: 1 nM - 10 μM
  • Incubation Time: 72 hours
  • Method:

    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)
Animal Research:

[1]
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  • Animal Models: HCT116 cells are injected s.c. Into the hind flank of male BALB/c mice.
  • Dosages: 15 mg/kg and 20 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

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(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing. 		5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 381.43
Formula

C19H23N7O2
CAS No. 896466-04-9
Storage powder
in solvent
Synonyms N/A
Smiles C1CC1NC(=O)NC2=C(NN=C2)C3=NC4=C(N3)C=C(C=C4)CN5CCOCC5

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Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID