1. Apoptosis
    Protein Tyrosine Kinase/RTK
  2. IAP
    FLT3
  3. LBW242

LBW242 

目录号: HY-15519
产品使用指南

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。

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LBW242 Chemical Structure

LBW242 Chemical Structure

CAS No. : 867324-12-7

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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].

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.
Molecular Weight

454.65

Formula

C₂₇H₄₂N₄O₂

CAS No.

867324-12-7

SMILES

[H][C@@]1(C2)[C@](CCN1C([C@H](C3CCCCC3)NC([C@H](C)NC)=O)=O)([H])CCN2CCC4=CC=CC=C4

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Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

LBW242LBW 242LBW-242IAPFLT3Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3multiplemyelomaantiapoptoticSmacmimeticMV4;11cellsmutantInhibitorinhibitorinhibit

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LBW242
目录号:
HY-15519
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