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LBW242

Catalog No. T15723   CAS 867324-12-7

LBW242 is a 3-mer and Smac mimetic and is an effective and orally active proapoptotic IAP inhibitor. LBW242 has activity against multiple myeloma and potentiates TRAIL- and anticancer drug-mediated cell death of ovarian cancer cells. LBW242 displays effects on mutant FLT3-expressing cells.

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LBW242 Chemical Structure
LBW242, CAS 867324-12-7
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 1,670.00
50 mg 6-8 weeks $ 2,180.00
100 mg 6-8 weeks $ 2,800.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description LBW242 is a 3-mer and Smac mimetic and is an effective and orally active proapoptotic IAP inhibitor. LBW242 has activity against multiple myeloma and potentiates TRAIL- and anticancer drug-mediated cell death of ovarian cancer cells. LBW242 displays effects on mutant FLT3-expressing cells.
In vitro 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 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. 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].
In vivo LBW242 (50 mg/kg; p.o.; daily for 10 days) decreases tumor burden[1].
Molecular Weight 454.65
Formula C27H42N4O2
CAS No. 867324-12-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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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Keywords

LBW242 867324-12-7 Others LBW 242 LBW-242 inhibitor inhibit

 

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