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LCL161

Chemical Structure : LCL161

CAS No.: 1005342-46-0

LCL161 (LCL-161)

货号: PC-20998Not For Human Use, Lab Use Only.

LCL161 is a monovalent Smac-mimetic, binds IAPs with high affinity and initiates the destruction of cIAP1 and cIAP2 (encoded by BIRC2 and BIRC3, respectively) and prevention of caspase inhibition by XIAP.

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5 mg ¥780 In stock
10 mg ¥1180 In stock
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50 mg ¥3280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

LCL161 is a monovalent Smac-mimetic, binds IAPs with high affinity and initiates the destruction of cIAP1 and cIAP2 (encoded by BIRC2 and BIRC3, respectively) and prevention of caspase inhibition by XIAP.
LCL161 modestly inhibits the growth of FLT3-ITD-expressing cells when administered alone, with an IC50 of 0.5 uM, show higher potencty against D835Y mutant with IC50 of 50 nM.
LCL161 significantly enhanced the ability of PKC412 to inhibit the growth of Ba/F3-FLT3-ITD-luc+ cells in vivo.
LCL161 in combination with radiotherapy led to dramatic tumor regression of HPV- HNSCC tumor xenografts, accompanied by cIAP1 degradation and apoptosis activation.

物理化学性质&存储条件

分子量 500.63
分子式 C26H33FN4O3S
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

(S)-N-((S)-1-cyclohexyl-2-((S)-2-(4-(4-fluorobenzoyl)thiazol-2-yl)pyrrolidin-1-yl)-2-oxoethyl)-2-(MethylaMino)propanaMide

参考文献

1. Weisberg E, et al. Leukemia. 2010 Dec;24(12):2100-9.

2. Linlin Yang, et al. Mol Cancer Ther. 2019 Jun;18(6):1025-1035.

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