LBW242

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LBW242 

LBW242， 是 3-mer 和 Smac 模拟物，一种有效的具有口服活性的促凋亡的 IAP 抑制剂。LBW242 对突变的 FLT3 细胞有抑制作用。LBW242 具有抗多发性骨髓瘤的活性， 并增强 TRAIL 和抗癌药物介导的卵巢癌细胞死亡。

LBW242

LBW242 Chemical Structure

CAS No. : 867324-12-7

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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 drug-mediated cell death of ovarian cancer cells[1][2].

体外研究
(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 1 μM[1].
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[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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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 .

体内研究
(In Vivo)

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

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

454.65

Formula

C27H42N4O2
CAS 号

867324-12-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

    [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.

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