DT-061

DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis[1].

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphatase

PP2A[1].

DT-061 (5 mg/kg, oral gavage, 4 weeks) shows single-agent activity in inhibiting H358 or H441 xenograft growth. Additionally, the combination of DT-061 and AZD6244 is more significantly efficient[1]. Animal Model: 6- to 8-week-old male BALB/c nu/nu mice injected with H441 cells (5 × 106)[1]. Dosage: 5 mg/kg. Administration: Oral gavage for 4 weeks. Result: Showed activity in inhibiting tumor growth.

[1]. Kauko O, et al. PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093.