Identification | Back 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 |
Hazard Information | Back 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.
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| [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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Company Name: |
SPIRO PHARMA
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Tel: |
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Website: |
www.spiropharma.com.cn |
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