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首页-小分子抑制剂&激动剂-Apoptosis-IAP-LBW242
LBW242

Chemical Structure : LBW242

CAS No.: 867324-12-7

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LBW242 (LBW-242)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 454.66
分子式 C27H42N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

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

参考文献

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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