产品名称
DT-061, ≥98% (HPLC)
Quality Level
SMILES string
O[C@H]1[C@@H](CCC[C@@H]1N2C3=C(OC4=C2C=CC=C4)C=CC=C3)NS(C5=CC=C(C=C5)OC(F)(F)F)(=O)=O
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Biochem/physiol Actions
Orally active, small molecule activator of PP2A (SMAP) with anti-cancer efficacy in cultures and in animals in vivo.
DT-061 is an orally active, small molecule activator of PP2A (NZ-8-061; SMAP1) that drives protein phosphatase 2 (PP2, PP2A) conformational changes by targeting the scaffold subunit Aα. DT-061 induces apoptotic death in cancer cultures (A549, H441, H358 IC50 ≤10 uM by MTT assay) and in mice in vivo (15 mg/kg with KRASLA2 transgenic model or 5 mg/kg with PDX tumor fragments or H358 xenograft model; via b.i.d. oral gavage) with little adverse effects to the animals.
DT-061 is an orally active, small molecule activator of PP2A (NZ-8-061; SMAP1) that drives protein phosphatase 2 (PP2, PP2A) conformational changes by targeting the scaffold subunit Aα. DT-061 induces apoptotic death in cancer cultures (A549, H441, H358 IC50 ≤10 uM by MTT assay) and in mice in vivo (15 mg/kg with KRASLA2 transgenic model or 5 mg/kg with PDX tumor fragments or H358 xenograft model; via b.i.d. oral gavage) with little adverse effects to the animals.
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