| Identification | Back Directory | [Name]
DT-061 | [CAS]
1809427-19-7 | [Synonyms]
Benzenesulfonamide, N-[(1R,2R,3S)-2-hydroxy-3-(10H-phenoxazin-10-yl)cyclohexyl]-4-(trifluoromethoxy)- | [Molecular Formula]
C25H23F3N2O5S | [MDL Number]
MFCD31813712 | [MOL File]
1809427-19-7.mol | [Molecular Weight]
520.52 |
| Chemical Properties | Back Directory | [Boiling point ]
625.5±65.0 °C(Predicted) | [density ]
1.51±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 125 mg/mL (240.14 mM);Water : < 0.1 mg/mL (insoluble) | [form ]
Solid | [pka]
10.48±0.60(Predicted) | [color ]
Off-white to light yellow | [SMILES]
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 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
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. |
| [storage]
Store at -20°C | [References]
[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. DOI:10.1126/scitranslmed.aaq1093 |
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