LBW242
Names
Biological Activity
[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]
Chemical & Physical Properties
[ Molecular Formula ]:
C27H42N4O2
[ Molecular Weight ]:
454.64800
[ Exact Mass ]:
454.33100
[ PSA ]:
64.68000
[ LogP ]:
3.48250