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Merck

SML4143

DT-061

≥98% (HPLC)

Synonym(s):

DT 061, DT061, SMAP, SMAP1, NZ-8-061, N-[(1R,2R,3S)-2-Hydroxy-3-(10H-phenoxazin-10-yl)cyclohexyl]-4-(trifluoromethoxy)benzenesulfonamide

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About This Item

Empirical Formula (Hill Notation):
C25H23F3N2O5S
CAS Number:
Molecular Weight:
520.52
MDL number:
NACRES:
NA.28
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Storage condition:
desiccated
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Quality Level

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

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

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.

Disclaimer

Hygroscopic


wgk

WGK 3

Storage Class

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable



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