Chemical Structure : LBW242
CAS No.:
867324-12-7
LBW242
(LBW-242)
Catalog No.: PC-20999Not For Human Use, Lab Use Only.
LBW242 (LBW-242) is a small molecule Smac-mimetic / inhibitor of apoptosis protein (IAP) antagonist, binds to XIAP (BIR3) with IC50 of 280 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
LBW242 (LBW-242) is a small molecule Smac-mimetic / inhibitor of apoptosis protein (IAP) antagonist, binds to XIAP (BIR3) with IC50 of 280 nM.
LBW242 inhibits growth and triggers apoptosis in MM cells (MM.1S, U266, RPMI-8226, and OPM2) with IC50 of 8-30 uM, without effect on normal lymphocytes and MM patient BMSCs.
LBW242 inhibits paracrine MM growth triggered by adherence to BMSCs, overcomes human IL-6 and IGF-1–mediated antiapoptotic effects and Bcl-2–mediated cytoprotective effects.
LBW242 (35 mg/kg, orally) for 2 weeks daily inhibits human plasmacytoma growth and prolongs survival in immune-deficient beige-nude-xid (BNX) mice.
LBW242 sensitizes XIAP-overexpressing neuroblastoma cells for TNF-α-independent apoptosis.
Physicochemical Properties
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M.Wt
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454.66
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Formula
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C27H42N4O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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C[C@H](NC)C(N[C@@H](C1CCCCC1)C(N2CC[C@]3([H])[C@@]2([H])CN(CCC4=CC=CC=C4)CC3)=O)=O
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References
1. Chauhan D, et al. Blood. 2007 Feb 1;109(3):1220-7.
2. Weisberg E, et al. Mol Cancer Ther. 2007 Jul;6(7):1951-61.
3. Gaither A, et al. Cancer Res. 2007 Dec 15;67(24):11493-8.
4. Eschenburg G, et al. Cancer Res. 2012 May 15;72(10):2645-56.
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