2. Cell Cycle/DNA Damage PI3K/Akt/mTOR Apoptosis
  3. ATM/ATR Apoptosis
  4. 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.

For research use only. We do not sell to patients.

ATM-IN-2 Chemical Structure

ATM-IN-2 Chemical Structure

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ATM-IN-2 Related Antibodies

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Description

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[1].

IC50 & Target[1]

ATM

4 nM (IC50)

In Vitro

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.

ATM-IN-2 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: HCT116 cells
Concentration: 1, 2, 4 μM
Incubation Time: 2 days
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. co-treated with Irinotecan.

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 1, 2, 4 μM
Incubation Time: 2 days
Result: The combined treatment group exhibited significantly higher apoptosis rates compared to monotherapy.

Western Blot Analysis[1]

Cell Line: HCT116 and SW620 cells
Concentration: 0.5, 1, 2 μM in HCT116 cells and 0.25, 0.5, 1 μM in SW620 cells
Incubation Time: 4 h
Result: Reduced the phosphorylation levels of ATM-S1981 and p53.
Reduced the accumulation of γH2AX.
Parmacokinetics[1]
Species Dose Route Indicator value
Mice 10 mg/kg i.v. Cmax 1460.9 ng/mL
Mice 10 mg/kg p.o. Tmax 1.32 h
Mice 10 mg/kg i.v. Tmax 0.08 h
Mice 10 mg/kg p.o. T1/2 4.1 h
Mice 10 mg/kg i.v. T1/2 4 h
Mice 10 mg/kg p.o. AUC0-t 14841.7 ng·h/mL
Mice 10 mg/kg i.v. AUC0-t 10055.3 ng·h/mL
Mice 10 mg/kg p.o. F 147.6 %
Mice 10 mg/kg p.o. Cmax 1285.8 ng/mL
In Vivo

ATM-IN-2 (Compound 25a) (15-30 mg/kg, p.o., for 14-20 days) exerts synergistic antitumor effects in cancer therapy with Irinotecan in mice xenograft model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Xenograft model induced by HCT116 or SW620 cells established in 6-weeks NOD-SCID mice[1]
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
Administration: Oral administration (p.o.), for 14 days in HCT116 model and 20 days for SW620 model
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.
Molecular Weight

443.52

Formula

C25H21N3O3S
SMILES

CC(S(=O)(C1=CC=C(C=C1)C2=CN=C3NC=C(C3=C2)C4=CC(C5=CC=CC=C5)=NO4)=O)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ATM-IN-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ATM-IN-2ATM/ATRApoptosisAtaxia telangiectasia mutatedATM and RAD3 relatedIrinotecanXenograft modelHCT116 cellsSW620 cellsBALB/c miceInhibitorinhibitorinhibit

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