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, and potentiates TRAIL- and anticancer drug-mediated cell death of ovarian cancer cells.
Product information
CAS Number: 867324-12-7
Molecular Weight: 454.65
Formula: C27H42N4O2
Chemical Name: (2S)-N-[(1S)-2-[(3aR,7aS)-6-(2-phenylethyl)-octahydro-1H-pyrrolo[2,3-c]pyridin-1-yl]-1-cyclohexyl-2-oxoethyl]-2-(methylamino)propanamide
Smiles: C[C@H](NC)C(=O)N[C@@H](C1CCCCC1)C(=O)N1CC[C@H]2CCN(C[C@@H]12)CCC1C=CC=CC=1
InChiKey: HCSMRSHIIKPNAK-LSAVBLLPSA-N
InChi: InChI=1S/C27H42N4O2/c1-20(28-2)26(32)29-25(23-11-7-4-8-12-23)27(33)31-18-15-22-14-17-30(19-24(22)31)16-13-21-9-5-3-6-10-21/h3,5-6,9-10,20,22-25,28H,4,7-8,11-19H2,1-2H3,(H,29,32)/t20-,22+,24+,25-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. 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.
In Vivo:
LBW242 (50 mg/kg; p.o.; daily for 10 days) reduces tumor burden.
Products are for research use only. Not for human use.
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