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  • DC Chemicals Limited
  • China
  • Product Name: LBW242
  • Price: ¥Inquiry/100mg ¥Inquiry/250mg ¥Inquiry/1g
  • Purity: 98.0%
  • Stocking Period: 1 Day
  • Contact: Tony Cao

867324-12-7

867324-12-7 structure
867324-12-7 structure
  • Name: LBW242
  • Chemical Name: 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)
  • CAS Number: 867324-12-7
  • Molecular Formula: C27H42N4O2
  • Molecular Weight: 454.64800
  • Catalog: Signaling Pathways Apoptosis IAP
  • Create Date: 2017-04-27 07:18:54
  • Modify Date: 2024-01-13 23:19:15
  • 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[1].

Name 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)
Synonyms lbw 242
Description 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[1].
Related Catalog
In Vitro LBW242 is a 3-mer and Smac mimetic, based on the ability of the NH2-terminal seven amino acids of Smac to neutralize the BIR3 domain of X-chromosome-linked IAP (XIAP). LBW242 partially inhibits the growth of mutant FLT3-expressing lines, MV4;11 at 1μM[1]. LBW242 (0-0.1 μM; 3 days) inhibits a panel of PKC412-sensitive or PKC412-resistant, mutant FLT3-expressing Ba/F3 lines The IC50 values ranged from 0.5 to >1 μM[1]. Cell Viability Assay[1] Cell Line: FLT3-ITD-Ba/F3 cells and mutant FLT3-expressing cells, A627T-FLT3-Ba/F3, F691IFLT3-Ba/F3, and N676D-FLT3-Ba/F3 cells Concentration: 0.001, 0.01, 0.1 μM Incubation Time: 3 days Result: Inhibited a panel of PKC412-sensitive or PKC412-resistant, mutant FLT3-expressing Ba/F3 lines The IC50 values ranged from 0.5 to >1 μM .
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.

Molecular Formula C27H42N4O2
Molecular Weight 454.64800
Exact Mass 454.33100
PSA 64.68000
LogP 3.48250