MU380 is a potent and selective CHK1 inhibitor that induces apoptosis and has anticancer activity[1].
Biological Activity
MU380 is a metabolically stable analog of CHK1 inhibitor SCH900776 (MK8776) does not undergo in vivo N-dealkylation. MU380 is a potent and selective CHK1 inhibitorwhich potently sensitizes multiple cancer cell lines to DNA antimetabolites including hydroxyureacytarabine and gemcitabine.
in vivo
MU380 (20 mg/kg, in 20% aqueous Kolliphor solution, every three days from day 14 to day 28) can effectively inhibit tumor growth in NOD-scid?IL2Rγnull?mice with tumour[1].
Animal Model:
NOD-scid?IL2Rγnull?mice[1]
Dosage:
20 mg/kg
Administration:
In 20% aqueous Kolliphor solution, every three days from day 14 to day 28
Result:
Significantly inhibit the growth of tumors and gradually reduce their volume, with an average reduction of about 61%.
References
[1] Miroslav Boudny, et al. Novel CHK1 inhibitor MU380 exhibits significant single-agent activity in TP53-mutated chronic lymphocytic leukemia cells. Haematologica. 2019 Dec;104(12):2443-2455. DOI:10.3324/haematol.2018.203430