产品
编 号：F610665
分子式：C27H42N4O2
分子量：454.65
分子式：C27H42N4O2
分子量：454.65
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CAS No: 867324-12-7
产品详情
生物活性：
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.
体内研究：
LBW242 (50 mg/kg; p.o.; daily for 10 days) reduces tumor burden.Animal Model:NCR nude mice were inoculated with FLT3-ITD-Ba/F3 cells
Dosage:50 mg/kg
Administration:Oral gavage; daily for 10 days
Result:Effective in reducing tumor burden.
体外研究：
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 1 μM. LBW242 kills cells in a manner strictly dependent on caspases, and death is accompanied by PARP cleavage, Annexin positivity, and accumulation of cells in sub-G1.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.
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.
体内研究：
LBW242 (50 mg/kg; p.o.; daily for 10 days) reduces tumor burden.Animal Model:NCR nude mice were inoculated with FLT3-ITD-Ba/F3 cells
Dosage:50 mg/kg
Administration:Oral gavage; daily for 10 days
Result:Effective in reducing tumor burden.
体外研究：
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 1 μM. LBW242 kills cells in a manner strictly dependent on caspases, and death is accompanied by PARP cleavage, Annexin positivity, and accumulation of cells in sub-G1.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.
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