| Hazard Information | Back Directory | [Uses]
Mps1-IN-5 is a potent and orally active Mps1 inhibitor with an IC50 value of 29 nM. Mps1-IN-5 induces Apoptosis and cell cycle arrests at G2/M phase. Mps1-IN-5 shows antiproliferative activity and anti-tumor activity. Mps1-IN-5 inhibits phosphorylation of Mps1 and induces DNA damage[1]. | [in vivo]
Mps1-IN-5 (30, 60 mg/kg; p.o.; daily for 15 days) inhibits tumor growth without obvious toxicity in breast cancer models[1]. | Animal Model: | 6-8 weeks, female BALB/C mice (4T1-luc mouse xenograft model)[1] | | Dosage: | 30, 60 mg/kg | | Administration: | P.o.; daily for 15 days | | Result: | Significantly suppressed tumor growth and caused negligible damage to organs such as heart, liver, spleen, lung and kidneys. |
| [References]
[1] Li X, et al. Design, synthesis and biological evaluation of a new class of 7H-pyrrolo[2,3-d]pyrimidine derivatives as Mps1 inhibitors for the treatment of breast cancer. Eur J Med Chem. 2023 Jan 5;245(Pt 1):114887. |
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