1. Cell Cycle/DNA Damage
    PI3K/Akt/mTOR
  2. ATM/ATR
  3. ATM Inhibitor-1

ATM Inhibitor-1 

Cat. No.: HY-112614
Handling Instructions

ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC50 of 0.7 nM, shows weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM) and PI3Kδ (IC50, 0.73 μM). ATM Inhibitor-1 exhibits anti-tumor activity.

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

ATM Inhibitor-1 Chemical Structure

ATM Inhibitor-1 Chemical Structure

CAS No. : 2135639-94-8

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Description

ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC50 of 0.7 nM, shows weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM) and PI3Kδ (IC50, 0.73 μM). ATM Inhibitor-1 exhibits anti-tumor activity[1].

IC50 & Target[1]

ATM

0.7 nM (IC50)

ATM

2.8 nM (IC50, Cellular assay)

PI3Kδ

0.73 μM (IC50)

PI3Kγ

3 μM (IC50)

PI3Kα

3.8 μM (IC50)

PI3Kβ

10.3 μM (IC50)

DNAPK

2.8 μM (IC50)

mTOR

21 μM (IC50)

In Vitro

ATM Inhibitor-1 (Compound 21) is a highly potent, selective and orally active ATM Inhibitor, with an IC50 of 0.7 nM, shows weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM) and PI3Kδ (IC50, 0.73 μM)[1].
In cellular assays, ATM Inhibitor-1 exhibits IC50s of 2.8 nM, >30 μM and >19 μM for ATM, ATR/PI3Kα and PI3Kβ/mTOR, respectively[1].

In Vivo

ATM Inhibitor-1 (Compound 21; 50 mg/kg p.o. once daily for 3 days every week starting 24 h post-irinotecan dosing, 21 days) in combination with 50 mg/kg irinotecan significantly reduces tumor growth in SW620 mice model[1].

Animal Model: SW620 mice model[1]
Dosage: 50 mg/kg
Administration: P.O., once daily for 3 days every week starting 24 h post-irinotecan dosing, 21 days
Result: Inhibited the growth of tumor combined with 50 mg/kg irinotecan in SW620 mice model.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Molecular Weight

492.61

Formula

C₂₇H₃₆N₆O₃

CAS No.

2135639-94-8

SMILES

C[[email protected]@H](C1CCOCC1)NC2=C(C(NC)=O)N=NC3=CC=C(C4=CC=C(OCCCN(C)C)N=C4)C=C32

Shipping

Room temperature in continental US; may vary elsewhere

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ATM Inhibitor-1
Cat. No.:
HY-112614
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ATM Inhibitor-1

Cat. No.: HY-112614