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867324-12-7

867324-12-7 Structure

867324-12-7 Structure
IdentificationBack Directory
[Name]

LBW242
[CAS]

867324-12-7
[Synonyms]

LBW242
LBW242,LBW-242
Propanamide, N-[(1S)-1-cyclohexyl-2-[(3aR,7aS)-octahydro-6-(2-phenylethyl)-1H-pyrrolo[2,3-c]pyridin-1-yl]-2-oxoethyl]-2-(methylamino)-, (2S)-
(2S)-N-[(1S)-2-[(3aR,7aS)-6-(2-phenylethyl)-3,3a,4,5,7,7a-hexahydro-2H-pyrrolo[2,3-c]pyridin-1-yl]-1-cyclohexyl-2-oxoethyl]-2-(methylamino)propanamide
[Molecular Formula]

C27H42N4O2
[MDL Number]

MFCD23160050
[MOL File]

867324-12-7.mol
[Molecular Weight]

454.65
Chemical PropertiesBack Directory
[Boiling point ]

645.2±55.0 °C(Predicted)
[density ]

1.098±0.06 g/cm3(Predicted)
[pka]

14.22±0.46(Predicted)
Hazard InformationBack Directory
[Uses]

LBW242, a 3-mer and Smac mimetic, is a potent and orally active proapoptotic IAP inhibitor. LBW242 shows effects on mutant FLT3-expressing cells. LBW242 has activity against multiple myeloma, and potentiates TRAIL- and anticancer agent-mediated cell death of ovarian cancer cells[1][2].
[in vivo]

LBW242 (50 mg/kg; p.o.; daily for 10 days) reduces tumor burden[1].

Animal Model:NCR nude mice were inoculated with FLT3-ITD-Ba/F3 cells[1]
Dosage:50 mg/kg
Administration:Oral gavage; daily for 10 days
Result:Effective in reducing tumor burden.
[References]

[1] Weisberg E, et al. Potentiation of antileukemic therapies by Smac mimetic, LBW242: effects on mutant FLT3-expressing cells. Mol Cancer Ther. 2007 Jul;6(7):1951-61. DOI:10.1158/1535-7163.MCT-06-0810
[2] Petrucci E, et al. A small molecule SMAC mimic LBW242 potentiates TRAIL- and anticancer drug-mediated cell death of ovarian cancer cells. PLoS One. 2012;7(4):e35073. DOI:10.1371/journal.pone.0035073
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