ATM-IN-2
ATM-IN-2 is a selective and orally active ATM inhibitor with an IC50 of 4 nM. ATM-IN-2 exhibits excellent kinase selectivity (>700-fold over PIKK family members). ATM-IN-2 exerts its anti-tumor effect by inhibiting ATM phosphorylation and the downstream signaling pathways (p53, H2AX), and promotes cell apoptosis. ATM-IN-2 can be used for the study of chemosensitizer candidate such as colon cancer.
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- Fòrmula: C25H21N3O3S
- Peso molecular:443.52
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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ATM 4 nM (IC50) |
ATM-IN-2 (Compound 25a) (0-10000 nM, 6-7 days) shows good inhibitory activity against HEL116 and SW620 cells, with IC50 values of 58.2 and 66.6 nM, and effectively inhibits the ability of cell clonal formation[1].
ATM-IN-2 (1-4 μM, 2 days) enhances the therapeutic efficacy of Irinotecan (HY-16562) by exacerbating G2/M phase arrest, and promoting apoptosis, and achieving synergistic antiproliferative effects in HCT116 cells[1].
ATM-IN-2 (0.25-2 μM, 4 h) significantly inhibits ATM signaling activation in HCT116 and SW620 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 cells
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Concentration:1, 2, 4 μM co-treated with Irinotecan (HY-16512)
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Incubation Time:2 days
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Result:Alone had no significant effect on the cell cycle.
Increased the G2/M phase population in a concentration-dependent manner accompanied by a reduction in the G0/G1 phase population.
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Cell Line:HCT116 cells
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Concentration:1, 2, 4 μM co-treated with Irinotecan
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Incubation Time:2 days
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Result:Exhibited significantly higher apoptosis rates compared to monotherapy.
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Cell Line:HCT116 and SW620 cells
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Concentration:0.5, 1, 2 μM in HCT116 cells and 0.25, 0.5, 1 μM in SW620 cells
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Incubation Time:4 h
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Result:Reduced the phosphorylation levels of ATM-S1981 and p53.
Reduced the accumulation of γH2AX.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Xenograft model induced by HCT116 or SW620 cells established in 6-weeks NOD-SCID mice[1]
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Dosage:30 mg/kg alone and 15 and 30 mg/kg with 2 mg/kg Irinotecan in HCT116 model; 45 mg/kg with 2 mg/kg Irinotecan in SW620 model
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Administration:Oral administration (p.o.), for 14 days in HCT116 model and 20 days for SW620 model
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Result:Demonstrated superior antitumor at high-dose coadministration with Irinotecan in HCT116 model.
Demonstrated a favorable safety profile with little body weight loss observed in HCT116 model.
Demonstrated a dose-dependent enhancement of inhibitory effects in SW620 model.
Chemical Information
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Peso molecular 443.52
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Fòrmula C25H21N3O3S
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SMILES
CC(S(=O)(C1=CC=C(C=C1)C2=CN=C3NC=C(C3=C2)C4=CC(C5=CC=CC=C5)=NO4)=O)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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