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Chemical Structure| 896466-04-9 Chemical Structure| 896466-04-9
Chemical Structure| 896466-04-9
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Product Details of AT9283

CAS No. :896466-04-9
Formula : C19H23N7O2
M.W : 381.43
SMILES Code : O=C(NC1CC1)NC1=CNN=C1C1=NC2=C(N1)C=CC(CN1CCOCC1)=C2
MDL No. :MFCD12031513
InChI Key :LOLPPWBBNUVNQZ-UHFFFAOYSA-N
Pubchem ID :135398495

Safety of AT9283

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of AT9283

epigenetics
DNA
RTK
JAK-STAT

Isoform Comparison

Biological Activity

Target
  • JAK3

    JAK3, IC50:1.1 nM

  • Tyk2

    TYK2, IC50:1 nM-10 nM

  • JAK2

    JAK2, IC50:1.2 nM

  • Aurora A

    Aurora A, IC50:~3.0 nM

In Vitro:

Cell Line
Concentration Treated Time Description Reference
HRCA-PDOs 0.1 μM 20 min To identify the live and dead cells and nucleus and determine the inhibitory efficacy. PMC10478412
human melanoma A375P cells 0.25 µM 24 hours To evaluate the effect of AT9283 on the proliferation and migration of A375P cells, results showed that AT9283 significantly inhibited cell proliferation and migration. PMC10932151
human melanoma A375P cells 0.25 µM, 0.5 µM, 0.75 µM, 1 µM 24 hours To evaluate the effect of AT9283 on the cell cycle of A375P cells, results showed that AT9283 induced G1/S phase cell cycle arrest. PMC10932151
A549 cells 0 nM, 125 nM, 250 nM, 500 nM 48 hours AT9283 significantly inhibited the proliferation of A549 cells, and DLGAP5 overexpression significantly reversed the AT9283-induced cell proliferation suppression. PMC10900829
H1299 cells 0 nM, 125 nM, 250 nM, 500 nM 48 hours AT9283 significantly inhibited the proliferation of H1299 cells, and DLGAP5 overexpression significantly reversed the AT9283-induced cell proliferation suppression. PMC10900829
HT29 cells 50 nM 72 h AT9283 significantly inhibited cell proliferation, promoted autophagy and cell death, and reduced MKK3 protein levels. PMC11334304
COLO205 cells 15 nM 72 h AT9283 significantly inhibited cell proliferation, promoted autophagy and cell death, and reduced MKK3 protein levels. PMC11334304
HCT116 cells 50 nM 72 h AT9283 significantly inhibited cell proliferation, promoted autophagy and cell death, and reduced MKK3 protein levels. PMC11334304
SW620 cells 100 nM 72 h AT9283 significantly inhibited cell proliferation, promoted autophagy and cell death, and reduced MKK3 protein levels. PMC11334304
SW480 cells 1.6 μM 72 h AT9283 significantly inhibited cell proliferation, promoted autophagy and cell death, and reduced MKK3 protein levels. PMC11334304
COLO320DM cells 885 nM 72 h AT9283 significantly inhibited cell proliferation, promoted autophagy and cell death, and reduced MKK3 protein levels. PMC11334304
CCD-18Co cells 4 μM 72 h AT9283 had minimal effects on primary colonocytes and did not significantly affect MKK3 protein levels. PMC11334304

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
BALB/c Nude mice H1299 cell xenograft model Intraperitoneal injection 20 mg/kg daily for 5 consecutive days, followed by a two-day interval, over a period of 3 weeks AT9283 significantly inhibited tumor growth in the H1299 cell xenograft model and significantly reduced the protein levels of DLGAP5 and PLK1 in the tumors. PMC10900829
Nude mice COLO205 xenograft model Gavage 15 mg/kg 5 days a week, until the end of the experiment AT9283 significantly inhibited COLO205 tumor growth and reduced MKK3 and AURKA protein levels. PMC11334304

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00985868 Unspecified Childhood Solid Tu... More >>mor, Protocol Specific Less << Phase 1 Active, not recruiting December 2018 United Kingdom ... More >> Birmingham Children's Hospital Birmingham, England, United Kingdom, B4 6NH Leeds General Infirmary Leeds, England, United Kingdom, LS9 7TF Royal Manchester Children's Hospital Manchester, England, United Kingdom, M27 4HA Great North Children's Hospital, Royal Victoria Infirmary Newcastle-Upon-Tyne, England, United Kingdom, NE1 4LP Royal Marsden - Surrey Sutton, England, United Kingdom, SM2 5PT Less <<
NCT01431664 Leukemia Phase 1 Completed - United Kingdom ... More >> Royal Marsden Hospital Surrey, London, United Kingdom, SM2 5PT Birmingham Children's Hospital Birmingham,, United Kingdom, B4 6NH Leeds General Infirmary Leeds, United Kingdom, LS1 3EX Royal Manchester Children's Hospital Manchester, United Kingdom, M13 9WL Great North Children's Hospital, Royal Victoria Infirmary Newcastle upon Tyne, United Kingdom, NE1 4LP Less <<
NCT00522990 Acute Myeloid Leukemia|Acute L... More >>ymphoblastic Leukemia|Chronic Myeloid Leukemia|Myelodysplastic Syndromes|Myelofibrosis Less << PHASE1|PHASE2 TERMINATED 2025-04-09 University of Alabama at Birmi... More >>ngham, Birmingham, Alabama, 35294, United States|The University of Texas, MD Anderson Cancer Center, Houston, Texas, 77030, United States Less <<
NCT00443976 Non-Hodgkins Lymphoma ... More >> Unspecified Adult Solid Tumor, Protocol Specific Less << Phase 1 Completed - Canada, British Columbia ... More >> BCCA - Vancouver Cancer Centre Vancouver, British Columbia, Canada, V5Z 4E6 Canada, Ontario Ottawa Health Research Institute - General Division Ottawa, Ontario, Canada, K1H 8L6 Less <<
NCT01145989 Multiple Myeloma PHASE2 COMPLETED 2015-11-27 Tom Baker Cancer Centre, Calga... More >>ry, Alberta, T2N 4N2, Canada|Cross Cancer Institute, Edmonton, Alberta, T6G 1Z2, Canada|Atlantic Health Sciences Corporation, Saint John, New Brunswick, E2L 4L2, Canada|QEII Health Sciences Center, Halifax, Nova Scotia, B3H 1V7, Canada|Juravinski Cancer Centre at Hamilton Health Sciences, Hamilton, Ontario, L8V 5C2, Canada|Univ. Health Network-Princess Margaret Hospital, Toronto, Ontario, M5G 2M9, Canada Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.62mL

0.52mL

0.26mL

13.11mL

2.62mL

1.31mL

26.22mL

5.24mL

2.62mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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