ATM Inhibitor-7 is a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor with an IC50 value of 1.0 nM. ATM Inhibitor-7 induces Apoptosis and cell cycle arrest at G2/M phase when combinanted with CPT-11 (HY-16562). ATM Inhibitor-7 combines with CPT-11 shows antitumor activity[1].
in vivo
ATM Inhibitor-7 (5 mg/kg; i.p.; once daily for 23 days) combines with CPT-11 (5 mg/kg, i.p.; once a week) shows antitumor activity in mice[1].
Animal Model:
Female nude mice (SW620 tumor xenograft model)[1]
Dosage:
5 mg/kg; CPT-11 (5 mg/kg, i.p.; once a week)
Administration:
I.p.; once daily for 23 days
Result:
Increased the antitumor activity of CPT-11.
IC 50
ATM: 1.0 nM (IC50)
References
[1] Shiyu Zhang, et al. Discovery of [1,2,3]Triazolo[4,5-c]quinoline Derivatives as a New Class of Ataxia-Telangiectasia Mutated Kinase Inhibitors. ACS Med. Chem. Lett. 2023.