ATM Inhibitor-1

Modify Date: 2024-01-11 12:35:29

ATM Inhibitor-1 Structure
ATM Inhibitor-1 structure
Common Name ATM Inhibitor-1
CAS Number 2135639-94-8 Molecular Weight 492.61
Density N/A Boiling Point N/A
Molecular Formula C27H36N6O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of ATM Inhibitor-1


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].

 Names

Name ATM Inhibitor-1

 ATM Inhibitor-1 Biological Activity

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].
Related Catalog
Target

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.
References

[1]. Barlaam B, et al. Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors. CS Med Chem Lett. 2018 Jul 13;9(8):809-814.

 Chemical & Physical Properties

Molecular Formula C27H36N6O3
Molecular Weight 492.61