867324-12-7
867324-12-7 structure
- Name: LBW242
- Chemical Name: Propanamide, N-[(1S)-1-cyclohexyl-2-[(3aR,7aS)-octahydro-6-(2-phenylethyl)-1H-pyrrolo[2,3-c]pyridin-1-yl]-2-oxoethyl]-2-(methylamino)-, (2S)
- CAS Number: 867324-12-7
- Molecular Formula: C27H42N4O2
- Molecular Weight: 454.64800
- Catalog: Signaling Pathways Apoptosis IAP
- Create Date: 2017-04-27 07:18:54
- Modify Date: 2024-01-13 23:19:15
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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].
| Name | Propanamide, N-[(1S)-1-cyclohexyl-2-[(3aR,7aS)-octahydro-6-(2-phenylethyl)-1H-pyrrolo[2,3-c]pyridin-1-yl]-2-oxoethyl]-2-(methylamino)-, (2S) |
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| Synonyms | lbw 242 |
| 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]. |
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| 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 |
| Molecular Formula | C27H42N4O2 |
|---|---|
| Molecular Weight | 454.64800 |
| Exact Mass | 454.33100 |
| PSA | 64.68000 |
| LogP | 3.48250 |