LCL161

For research use only. Not for use in humans.

目录号：S7009

LCL161 Chemical Structure

CAS No. 1005342-46-0

LCL-161, 一种second mitochondrial activator of caspase (SMAC, 线粒体促凋亡蛋白)模拟物, 能有效地结合并抑制多种IAPs(i.e. XIAP, c-IAP)。

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RMB 1194.96 现货
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客户使用Selleck生产的LCL161发表文献25篇：

产品安全说明书

IAP抑制剂选择性比较

生物活性

产品描述 LCL-161, 一种second mitochondrial activator of caspase (SMAC, 线粒体促凋亡蛋白)模拟物, 能有效地结合并抑制多种IAPs(i.e. XIAP, c-IAP)。
靶点
cIAP [1] XIAP [1]
体外研究

LCL161以高亲和力与凋亡抑制蛋白因子(IAPs)结合，并启动对cIAP1和cIAP2的破坏，其通过胱天蛋白酶的激活进一步诱导细胞凋亡。LCL161单独给药时适度抑制表达FLT3-ITD的细胞生长，IC50的范围为~0.5 μM (Ba/F3-FLT3-ITD 细胞)到~4 μM (MOLM13-luc+ 细胞)。观察到的LCL161抗D835Y突变体的效力相当高，测试抗Ba/F3-D835Y细胞时，IC50为~50 nM。LCL161 与PKC412结合治疗MOLM13-luc+细胞比其任何一个药剂单独使用具有更显著的细胞杀伤力，Calcusyn复合指数表明其具有协同作用。 PKC412和LCL161诱导MOLM13-luc+细胞的凋亡。PKC412 和 LCL161结合比其单独使用能够导致更高的细胞凋亡率。LCL161通过与PKC412阳性结合，抑制基质介导的表达FLT3的突变细胞的存活。LCL161抑制Ba/F3.p210细胞的生长，IC50为~100 nM。LCL161与ABL抑制剂，伊马替尼结合，能够协同抗BCR-ABL表达的细胞。对于在靶蛋白表达点突变的耐药细胞，LCL161也具有抵抗活性。1000 nM的LCL161能够大部分或完全杀死耐PKC412的Ba/F3衍生的细胞系，其在FLT3的ATP结合囊表达含有点突变的FLT3-ITD。100到1000 nM浓度的LCL161也表现出抗Ba/F3细胞的活性， Ba/F3细胞能够表达各种伊马替尼和尼罗替尼耐药的BCR-ABL点突变。[1] 对LCL161抗23细胞系的评估，通过儿科临床前测试计划(PPTP)在体外进行96小时。对23种测试PPTP细胞系中的其中3种，10 μM浓度下的LCL161能够抑制50%的生长。3种细胞系包括2种T细胞ALL细胞系(COG-LL-317和CCRF-CEM)，以及间变性大细胞淋巴瘤细胞系(Karpas-299)，CCRF-CEM和Karpas-299表现出较低的相对IC50值(分别为0.25和1.6 μM)。[2] LCL161对人体免疫亚群表现出免疫调节性能。用LCL161处理T淋巴细胞显著增强具有激活作用的细胞因子分泌，对 CD4和CD8 T细胞生存或分化的作用很小。LCL161处理外周血单核细胞，在体外合成多肽存在下，显著增强初始T细胞的启动。髓样树突状细胞在LCL161作用下表型成熟，表明降低了基于肿瘤抗原对抗疫苗的能力。这些作用可能通过观察到的典型和非典型NF-κB途径的激活介导，伴随LCL161导致抗凋亡分子上调。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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H460 Ml;PSpVv[3Srb36gZZN{[Xl? NX7XS5J3Oy5|IIXN Ml72OUBl[Xm| MoWyVI91\W62aXH0bY9vKG:oIHPvcoF1fW23bXHiMYlv\HWlZXSgZ5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTFQ3OCClZXzsd{BifCB|LkOgeW0h[W[2ZYKgOUBl[Xm|IHL5JG1VWyCjc4PhfS=> NXzTb3dXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFM4QDJpPkK0NFg{Pzh{PD;hQi=>
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MDA-MB-231 NGXNUppHfW6ldHnvckBie3OjeR?= MX2wMlM4KHSxIEOuN{B2VQ>? NV3qXHNyOTliaILz NFz6PIlKdmirYnn0bY9vKG:oIHPJRXAyNzJiaX6gbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjc4Pld5Nm\CCjczDpcoR2[3Srb36gc4YhXE6IYXzwbIEhdGW4ZXygZZQhOC5|NzD0c{A{NjNidV2gZYZ1\XJiMUmgbJJ{KGK7IFXMTXNC M4LUNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEmzPVQxLz5{NEC5N|k1ODxxYU6=
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MDA-MB-231 M1;3bmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NVXiWFdlPzJiaILz NX;K[Id1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCDbHHtZZIh[my3ZTDhd5NigSxiSVO1NEA:KDBwMEC3PEDPxE1w MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB7MU[wNEc,OzByOUG2NFA9N2F-
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SKOV3 MUfBdI9xfG:|aYOgZZN{[Xl? NUDTUY5iPDhiaILz NFXIPZpKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIGPLU3Y{KGOnbHzzJIF{e2W|c3XkJINie3Cjc3WtN{Bi[3SrdnH0bY9vKGGodHXyJFQ5KGi{czDifUBKdmO3Q4n0[UBUOyCuaY\lMYNmdGxiYX7hcJl{cXNuIFXDOVAhRSByLkCwNUDPxE1w M1P2O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzMEm1N|g3Lz5|MUC5OVM5PjxxYU6=
SKOV3 MX7BdI9xfG:|aYOgZZN{[Xl? MkXENlQhcHK| MlnYTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCVS1;WN{Bk\WyuczDhd5Nme3OnZDDjZZNx[XOnLUOgZYN1cX[jdHnvckBi\nSncjCyOEBpenNiYomgTY5kfUO7dHWgV|MhdGm4ZT3j[YxtKGGwYXz5d4l{NCCHQ{WwJF0hOC5yMEOg{txONg>? M4nkc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzMEm1N|g3Lz5|MUC5OVM5PjxxYU6=
BL21(DE3) MVvGeY5kfGmxbjDhd5NigQ>? NXLQbYR3OiCqcoO= NHHQO4hFcXOybHHj[Y1mdnRib3[gZolwfGmweXzheIVlKEGYUF[g[pJwdSCQLYTldo1qdmGuIFjpd{B1[WepZXSgdoVkd22kaX7hcpQhcHWvYX6gXGlCWC2ESWKzJIRwdWGrbjCoNlU{KHSxIEO0O{Bz\XOrZIXld{kh\XiycnXzd4VlKGmwIFXzZ4hmemmlaHnhJINwdGliQlyyNUhFTTNrIHPlcIx{KGmwY4XiZZRm\CCob4KgNkBpenNiYomgSGVNTkmDLDDJR|UxKD1iMD6wOFgh|ryPLh?= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTB7NUO4Okc,OzFyOUWzPFY9N2F-
BL21(DE3) M4LkOWZ2dmO2aX;uJIF{e2G7 MX[4JIhzew>? NUDvcnN[TGm|cHzhZ4Vu\W62IH;mJIJqd3SrbonsZZRm\CCDVmDGJIZzd21iTj30[ZJucW6jbDDIbZMhfGGpZ3XkJJJm[2:vYnnuZY51KGi3bXHuJHhKSVBvQlnSN{Bld22jaX6gLFI2OyC2bzCzOFchemW|aXT1[ZMqKGW6cILld5Nm\CCrbjDFd4Np\XKrY3jpZUBkd2yrIFLMNlEpTEV|KTDj[YxteyCrbnP1ZoF1\WRiZn;yJFghcHK|IHL5JGRGVE[LQTygTWM2OCB;IECuNFU{KM7:TT6= M1PlelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzMEm1N|g3Lz5|MUC5OVM5PjxxYU6=
A549 NHT2bHpHfW6ldHnvckBie3OjeR?= M4OyW|EhfU1? MljmN{BpenN? NFTCPJdKdmS3Y4Tpc44hd2ZiY1nBVFIh\GWpcnHkZZRqd25iaX6gbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY1nBVFIheHKxdHXpckBt\X[nbDDheEAyKHWPIHnuZ5Vj[XSnZDDmc5IhOyCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTV3MEG1OUc,OzF3NUCxOVU9N2F-
SK-MEL-28 NWru[m5XTnWwY4Tpc44h[XO|YYm= MnnINUB2VQ>? MUOzJIhzew>? NETHdHBKdmS3Y4Tpc44hd2ZiY1nBVFEh\GWpcnHkZZRqd25iaX6gbJVu[W5iU1utUWVNNTJ6IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBkUUGSMTDwdo91\WmwIHzleoVtKGG2IEGgeW0hcW6ldXLheIVlKG[xcjCzJIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> NV7rdo5KRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G1OVAyPTVpPkOxOVUxOTV3PD;hQi=>
SK-MEL-28 MX\GeY5kfGmxbjDhd5NigQ>? NH[2SI8yKHWP NUDkUXhJOyCqcoO= MUTJcoR2[3Srb36gc4Yh[0mDUEKg[IVoemGmYYTpc44hcW5iaIXtZY4hW0tvTVXMMVI5KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDjTWFROiCycn;0[YlvKGyndnXsJIF1KDFidV2gbY5kfWKjdHXkJIZweiB|IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= MoHsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF3NUCxOVUoRjNzNUWwNVU2RC:jPh?=
HEK293T MVPGeY5kfGmxbjDhd5NigQ>? MXixNEB2VQ>? NH64dYs3KGi{cx?= M1S4ZmNwfmGuZX70JIJqdmSrbnegZYZncW6rdImgeI8hUEFvQlnSN{Bld22jaX6gc4YhYEmDUDCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBJTUt{OUPUJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGKjbnSgbY51\W6|aYT5JIF1KDFyIIXNJIlv[3WkYYTl[EBnd3JiNjDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz M4qzS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUWwNVU2Lz5|MUW1NFE2PTxxYU6=
A549 M2D3VmZ2dmO2aX;uJIF{e2G7 NH\U[mQyKHWP MV6zJIhzew>? Mk\OTY5lfWO2aX;uJI9nKGOLQWCxJIRm\3KjZHH0bY9vKGmwIHj1cYFvKEF3NEmgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOLQWCxJJBzd3SnaX6gcIV3\WxiYYSgNUB2VSCrbnP1ZoF1\WRiZn;yJFMhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MofhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF3NUCxOVUoRjNzNUWwNVU2RC:jPh?=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
cIAP1 / cIAP2 / XIAP / surivivin ; 

PubMed: 27737687     


A549 and H460 cells were treated for 48 h with 0-20 μM LCL161. The protein levels of cIAP1, cIAP2, XIAP and survivin were assessed by western blotting. β-actin was used as a loading control. The bar graphs represent the mean ± SD of different proteins/β-actin; *P < 0.05; **P < 0.01; ***P < 0.001

27737687
Growth inhibition assay
Cell viability; 

PubMed: 27737687     


Cells were treated for 48 h with the indicated concentrations of LCL161 and paclitaxel (c) or for the indicated times with 10 μM LCL161 and/or 10 μM paclitaxel (d). Cell viability was determined by the MTT assay. Data are represented as mean ± SD; *P < 0.05; **P < 0.01; ***P < 0.001

27737687
体内研究 LCL161显著增强PKC412抑制Ba/F3-FLT3-ITD-luc+细胞体内生长的能力。LCL161能够与标准化疗剂，阿糖胞苷和阿霉素阳性结合，抗FLT3-ITD表达细胞和D835Y表达细胞。Nilotinib与LCL161结合能够实现抑制白血病生长的累加作用。LCL161 (100 毫克/千克)增强高适度剂量nilotinib (100毫克/千克)对患有白血病小鼠的体内作用。[1] 通过儿科临床前测试程序(PPTP)测试CL161(口服给药，一周两次)在体内(30 或 75 毫克/千克[实体瘤] 或100 毫克/千克 [ALL])的作用。LCL161诱导显著的EFS在大约三分之一实体瘤异种移植物(osteosarcoma and glioblastoma) 中的分布差异，但不影响ALL异种移植物中的情况。没有观察到可评价客观疗效者。在体内，LCL161对儿科临床前模型研究表现出有限的单剂量活性。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验：

[1]
- 合并
  • Cell lines: 人 T 细胞 ALL 细胞系 COG-LL-317
  • Concentrations: ~10 μM
  • Incubation Time: 96小时
  • Method:

    使用DIMSCAN进行体外测试


    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (199.74 mM)
Water Insoluble
Ethanol '20 mg/mL warmed

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 500.63
化学式

C26H33FN4O3S
CAS号 1005342-46-0
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量 只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量：

总分子量：g/mol

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03111992 Completed Drug: PDR001|Drug: CJM112|Drug: LCL161 Multiple Myeloma Novartis Pharmaceuticals|Novartis December 18 2017 Phase 1
NCT01934634 Unknown status Drug: LCL161|Drug: Gemcitabine|Drug: nab-Paclitaxel Metastatic Pancreatic Cancer US Oncology Research|Novartis Pharmaceuticals|Delta Clinical Research LLC March 2014 Phase 1
NCT01968915 Completed Drug: LCL161|Drug: Paclitaxel Neoplasms Novartis Pharmaceuticals|Novartis November 2013 Phase 1
NCT01617668 Completed Drug: LCL161|Drug: paclitaxel Breast Cancer Novartis Pharmaceuticals|Novartis August 2012 Phase 2

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

  • * 必填项
Selleck产品目录册

IAP Signaling Pathway Map
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID