產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 10mg 50mg 100mg
CAS	1005342-46-0
別名	LCL-161;LCL 161
化學(xué)名	(2S)-N-[(1S)-1-cyclohexyl-2-[(2S)-2-[4-(4-fluorobenzoyl)-1,3-thiazol-2-yl]pyrrolidin-1-yl]-2-oxoethyl]-2-(methylamino)propanamide
分子式	C26H33FN4O3S
分子量	500.63
溶解度	≥ 25.05 mg/mL in DMSO
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

LCL161 is a small molecular antagonist of the inhibitor of apoptosis (IAP) with IC50 value of 10.23 μM in Hep3B cells [1].

IAP is a family of proteins which are firstly found in virus and to inhibit the apoptosis of the infected hosts. It contains eight proteins in human. Since they were always found to overexpress in variety of malignant tumors, the IAP are thought to be appropriate targets in cancer therapy. SMAC (second mitochondria-derived activator of caspases) is the first-identified antagonist of IAP. It binds to XIAP within the BIR2/3 domain through its N-terminal segment. As a mimetic of SMAC, LCL161 is designed to be the inhibitor of both XIAP and cIAP1/2 [1].

LCL161 showed significant inhibition of cell proliferation and viability in two human hepatocellular carcinoma (HCC) cells, Hep3B and PLC5. The IC50 values were 10 and 19 μM, respectively. However, LCL161 had no effect in the two other HCC cell lines, Sk-Hep1 (IC50 value of 224 μM) and Huh-7 (IC50 value of 228 μM). The difference of the effects is found to dependent on the expression of Bcl-2 in cells. For the ALL cells, LCL161 exerted growth inhibition with IC50 values of 9.3 and 0.25 μM, respectively. LCL161 also showed effect on the ALCL cell line Karpas-299 with IC50 value of 1.6 μM [1, 2].

In vivo, LCL161 markedly affected the distribution of EFS in many solid tumor xenograft models. It also caused growth delay in some tumors such as osteosarcoma, neuroblastoma and glioblastoma at dose of 30 mg/kg orally. Besides that, LCL161 administration caused significant growth inhibition in EW-5 and BT-39 glioblastoma but not in BT-28. Moreover, the combination therapy of LCL161 and the adeno-associated virus bacteriophage-tumor necrosis factor-α (AAVP-TNF-α) has been reported to has synergistic anti-tumor effects and delayed treatment resistance in mice models of tumor xenografts [1, 2 and 3].

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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