LCL161

目录号:S7009

仅限科研使用

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)。

LCL161 Chemical Structure

CAS: 1005342-46-0

规格 价格 库存 购买数量
RMB 1194.96 现货
RMB 3883.15 现货
RMB 8176.93 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的LCL161发表文献29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
LOX Mk\2SpVv[3Srb36gZZN{[Xl? NHPjZ3UyODBibXevb4c> NIrveXo5KGi{cx?= M4WzenBwfGWwdHnheIlwdiCxZjDjc45ifHWvdX3hZk1qdmS3Y3XkJINKSVBzIHTl[5Ji\GG2aX;uJIlvKGi3bXHuJGxQYCClZXzsd{B5\W6xZ4Lh[pRm\CCrbjDtc5V{\SCjdDCxNFAhdWdxa3esJJBwKGGodHXyJFghcHK|IHL5JHdme3Sncn6gZoxwfHSrbnegZY5idHm|aYO= MnX5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEO3PFIoRjJ2MEizO|gzRC:jPh?=
LOX M1m1PGZ2dmO2aX;uJIF{e2G7 Mn;IPEBpenN? MXTQc5RmdnSrYYTpc44hd2ZiY3;uZZR2dXWvYXKtbY5lfWOnZDDjZZNx[XOnIEOvO{Bi[3SrdnH0bY9vKGmwIHj1cYFvKEyRWDDj[YxteyC6ZX7v[5Ji\nSnZDDpckBud3W|ZTDh[pRmeiB6IHjyd{BjgSCobIXvdoV{[2WwY3WgZZN{[Xl? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB6M{e4Nkc,OjRyOEO3PFI9N2F-
MDA-MB-231 MVjGeY5kfGmxbjDhd5NigQ>? NXzGboFKOi53IITvJFExKHWP MW[xPUBpenN? M1jiZWJqdmSrbnegZYZncW6rdImgeI8h[0mDUEGgRmlTOyCmb33hbY4hcW5iaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDUUmZidHCqYTDs[ZZmdCCjdDCyMlUhfG9iMUCgeW0h[W[2ZYKgNVkhcHK|IHL5JGVNUVOD M3jBNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEizO|gzLz5{NEC4N|c5OjxxYU6=
BxPC3 MVrGeY5kfGmxbjDhd5NigQ>? MoGxN{4{KHWP M2LLVlUh\GG7cx?= NHTJWHhRd3SnboTpZZRqd25ib3[gZ49v[XS3bYXtZYIucW6mdXPl[EBkgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDgFCFMzDj[YxteyCjdDCzMlMhfU1iYX\0[ZIhPSCmYYnzJIJ6KE2WUzDhd5NigQ>? MlrIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEO3PFIoRjJ2MEizO|gzRC:jPh?=
HCT15 MUnGeY5kfGmxbjDhd5NigQ>? MWezMlMhfU1? MnjwOUBl[Xm| NEnBfHlRd3SnboTpZZRqd25ib3[gZ49v[XS3bYXtZYIucW6mdXPl[EBkgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzNTDj[YxteyCjdDCzMlMhfU1iYX\0[ZIhPSCmYYnzJIJ6KE2WUzDhd5NigQ>? NX3RN4FNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFM4QDJpPkK0NFg{Pzh{PD;hQi=>
SW620 M4LHWWZ2dmO2aX;uJIF{e2G7 NVrnVVZzOS5zIIXN NH\SN3Y2KGSjeYO= MmnCVI91\W62aXH0bY9vKG:oIHPvcoF1fW23bXHiMYlv\HWlZXSgZ5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV3c3OjBiY3XscJMh[XRiMT6xJJVOKGGodHXyJFUh\GG7czDifUBOXFNiYYPzZZk> M3rIeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEizO|gzLz5{NEC4N|c5OjxxYU6=
SW620 M36yR2Z2dmO2aX;uJIF{e2G7 M2HHdFMvOyC3TR?= MnfhOUBl[Xm| NVG4UotrWG:2ZX70bYF1cW:wIH;mJINwdmG2dX31cYFjNWmwZIXj[YQh[3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW1d4MkCgZ4VtdHNiYYSgN{4{KHWPIHHmeIVzKDViZHH5d{BjgSCPVGOgZZN{[Xl? NHLxTVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4N|c5Oid-MkSwPFM4QDJ:L3G+
LOX NUHEZYlJTnWwY4Tpc44h[XO|YYm= MX:zMlMhfU1? MWqzJIRigXN? NGLYOnlRd3SnboTpZZRqd25ib3[gZ49v[XS3bYXtZYIucW6mdXPl[EBkgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNV1hiY3XscJMh[XRiMz6zJJVOKGGodHXyJFMh\GG7czDifUBOXFNiYYPzZZk> MkHVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEO3PFIoRjJ2MEizO|gzRC:jPh?=
LS180 NIrl[|RHfW6ldHnvckBie3OjeR?= NXvCXG17Oy5|IIXN M176flUh\GG7cx?= Mly5VI91\W62aXH0bY9vKG:oIHPvcoF1fW23bXHiMYlv\HWlZXSgZ5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUHMyQDBiY3XscJMh[XRiMz6zJJVOKGGodHXyJFUh\GG7czDifUBOXFNiYYPzZZk> NFjSc3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4N|c5Oid-MkSwPFM4QDJ:L3G+
H460 M3X2TmZ2dmO2aX;uJIF{e2G7 MkDCN{4{KHWP M2LlSlUh\GG7cx?= MmHlVI91\W62aXH0bY9vKG:oIHPvcoF1fW23bXHiMYlv\HWlZXSgZ5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTFQ3OCClZXzsd{BifCB|LkOgeW0h[W[2ZYKgOUBl[Xm|IHL5JG1VWyCjc4PhfS=> NUPmcplHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFM4QDJpPkK0NFg{Pzh{PD;hQi=>
LOX NHn5d2lHfW6ldHnvckBie3OjeR?= MX6xNFAhdWdxa3e= M4TlfFghcHK| NV3U[nJ4WGyjc33hJINwdmOnboTyZZRqd25iaX6gcpVl\SCvb4Xz[UB5\W6xZ4Lh[pRm\CC5aYToJIh2dWGwIFzPXEBk\WyuczDheEAyODBibXevb4ctKHCxIH3lZZN2emWmIHH0JFghcHK|LDDDdEA:KDNwMzFOwG0v M4jhclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEmzPVQxLz5{NEC5N|k1ODxxYU6=
SW620 NFT3bZFHfW6ldHnvckBie3OjeR?= M4Do[VUh\GG7cx?= MYHJcoR2[3Srb36gc4Yhe2Wwc3n0bZpifGmxbjDv[kBpfW2jbjDTW|YzOCClZXzsd{B1dyClb37heJVufW2jYj3pcoR2[2WmIHHwc5B1d3OrczDhd5Nme3OnZDDhd{Bk\WyuII\pZYJqdGm2eTDh[pRmeiB3IHThfZMh[nliTWTTJIF{e2G7LDDFR|kxKD1iNj62OkDPxE1w MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB7M{m0NEc,OjRyOUO5OFA9N2F-
LOX NW\GfVMzTnWwY4Tpc44h[XO|YYm= NWjJXoFiOTByIH3nM4to MkfsPEBpenN? NGPpNYxFenWpIIXweIFs\SCrbjD0eY1weiCxZjDueYRmKG2xdYPlJJhmdm:pcnHmeIVlKHerdHigbJVu[W5iTF;YJINmdGy|IHH0JFExOCCvZz;r[{wheG9ibXXhd5Vz\WRiYYSgPEBpenNuIFTyeYchfXC2YXvlJF0hOThwNDFOwG0v M3TWSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEmzPVQxLz5{NEC5N|k1ODxxYU6=
SW620 NX36UW9DTnWwY4Tpc44h[XO|YYm= M17ZTlIvPSC3TR?= M1HRUFUh\GG7cx?= Ml\uTY5lfWO2aX;uJI9nKHOnboPpeIl7[XSrb36gc4YhcHWvYX6gV3c3OjBiY3XscJMhfG9iY3;uZZR2dXWvYXKtbY5lfWOnZDDhdI9xfG:|aYOgZZN{\XO|ZXSgZZMh[2WubDD2bYFjcWyrdImgZZQhOi53IIXNJIFnfGW{IEWg[IF6eyCkeTDNWHMh[XO|YYm= M37lW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEmzPVQxLz5{NEC5N|k1ODxxYU6=
LOX MkToSpVv[3Srb36gZZN{[Xl? M2XFOVExOCCvZz;r[y=> MnrCPEBpenN? Mn7LTY4hfmm4bzDpcohq[mm2aX;uJI9nKFiLQWCgRmlTOiCmb33hbY4hcW5iaIXtZY4hVE:[IHPlcIx{KHinbn;ndoFnfGWmIHnuJI52\GVibX;1d4Uh[XO|ZYPz[YQh[XNicH;0[Y51cWG2aX;uJI9nKGOxbnH0eY12dWGkLXnu[JVk\WRiY3HzdIF{\SB|L{egZYN1cX[rdImgZZQhOTByIH3nM4toNCCybzDh[pRmeiB6IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= NGHtTnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC5N|k1OCd-MkSwPVM6PDB:L3G+
LOX M{fqdmZ2dmO2aX;uJIF{e2G7 MWmxNFAhdWdxa3e= NI[2VW05KGi{cx?= NVXMR5RZUW5idnn2c{BqdmirYnn0bY9vKG:oIGjJRXAhSkmUMjDkc41icW5iaX6gbJVu[W5iTF;YJINmdGy|IIjlco9oemGodHXkJIlvKG63ZHWgcY92e2ViYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4h[2G|cHHz[UA{NzdiYXP0bZZqfHliYYSgNVAxKG2pL3vnMEBxdyCjZoTldkA5KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? M2TTcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEmzPVQxLz5{NEC5N|k1ODxxYU6=
MDA-MB-231 NWW4cI1ETnWwY4Tpc44h[XO|YYm= NIjhTXIxNjN5IITvJFMvOyC3TR?= MUKxPUBpenN? MVzJcohq[mm2aX;uJI9nKGOLQWCxM|IhcW5iaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bie3Onc4Pl[EBieyCrbnT1Z5Rqd25ib3[gWG5H[WyyaHGgcIV3\WxiYYSgNE4{PyC2bzCzMlMhfU1iYX\0[ZIhOTliaILzJIJ6KEWOSWPB Ml2zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOUO5OFAoRjJ2MEmzPVQxRC:jPh?=
CHL1 MXXGeY5kfGmxbjDhd5NigQ>? NXHzenZrOC52IITvJFExKHWP MlK3NlghcHK| NYXtTHFRUW6qaXLpeIlwdiCxZjDjTWFROSCrbjDoeY1idiCFSFyxJINmdGy|IHH0JFAvPCC2bzCxNEB2VSCjZoTldkAzQCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| NUfkUIoxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPVM6PDBpPkK0NFk{QTRyPD;hQi=>
SKMES1 MWfGeY5kfGmxbjDhd5NigQ>? NYLVb5VwOi53IIXN MWi1JIRigXN? MmD6VI91\W62aXH0bY9vKG:oIHPvcoF1fW23bXHiMYlv\HWlZXSgZZBweHSxc3nzJIlvKGi3bXHuJHNMVUWVMTDj[YxteyCjdDCyMlUhfU1iYX\0[ZIhPSCmYYnzJIJ6KE2WUzDhd5NigQ>? NGjIbnE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC5N|k1OCd-MkSwPVM6PDB:L3G+
Capan1 NGPBWJhHfW6ldHnvckBie3OjeR?= NWX5O4R7Oi53IIXN NUThUHpxPSCmYYnz NWKwc402WG:2ZX70bYF1cW:wIH;mJINwdmG2dX31cYFjNWmwZIXj[YQh[XCxcITvd4l{KGmwIHj1cYFvKEOjcHHuNUBk\WyuczDheEAzNjVidV2gZYZ1\XJiNTDkZZl{KGK7IF3UV{Bie3OjeR?= M{HYe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEmzPVQxLz5{NEC5N|k1ODxxYU6=
AGS NXPqb4o5TnWwY4Tpc44h[XO|YYm= MoDmNk42KHWP NEjEfWQ2KGSjeYO= NVzYc5d6UW6mdXP0bY9vKG:oIIPlcpNqfGm8YYTpc44hd2ZiaIXtZY4hSUeVIHPlcIx{KHSxIHPvcoF1fW23bXHiMYlv\HWlZXSgZZBweHSxc3nzJIF{e2W|c3XkJIF{KGOnbHygeoli[mmuaYT5JIF1KDJwNTD1UUBi\nSncjC1JIRigXNiYomgUXRUKGG|c3H5 NHXuVWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC5N|k1OCd-MkSwPVM6PDB:L3G+
U118MG M4PFZmZ2dmO2aX;uJIF{e2G7 NX7sZ3VtOi53IIXN NVPZ[2RqPSCmYYnz MoX2VI91\W62aXH0bY9vKG:oIHPvcoF1fW23bXHiMYlv\HWlZXSgZZBweHSxc3nzJIlvKGi3bXHuJHUyOTiPRzDj[YxteyCjdDCyMlUhfU1iYX\0[ZIhPSCmYYnzJIJ6KE2WUzDhd5NigQ>? M4nrOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEmzPVQxLz5{NEC5N|k1ODxxYU6=
PC3 M1L6[mZ2dmO2aX;uJIF{e2G7 MYOyMlUhfU1? MorZOUBl[Xm| MoXZTY5lfWO2aX;uJI9nKHOnboPpeIl7[XSrb36gc4YhcHWvYX6gVGM{KGOnbHzzJJRwKGOxbnH0eY12dWGkLXnu[JVk\WRiYYDvdJRwe2m|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHH0JFIvPSC3TTDh[pRmeiB3IHThfZMh[nliTWTTJIF{e2G7 MnnUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOUO5OFAoRjJ2MEmzPVQxRC:jPh?=
CCRF-CEM MnfyRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NXGyd41oSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDR3JHNUOHTTDj[YxteyxiR1m1NEA:KDBwMkWg{txONg>? MoTBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2M{W1NlYoRjJ6NEO1OVI3RC:jPh?=
MDA-MB-231 MlHJSpVv[3Srb36gZZN{[Xl? NHzNXHYzKGi{cx?= M4TReWlv\HWldHnvckBw\iClSVHQNUBl\We{YXTheIlwdiCrbjDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGGodHXyJFIhcHK|LDDFR|UxKD1iMD6wNFA1KM7:TT6= NVXIOY57RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0PVI{OTdpPkK4OFkzOzF5PD;hQi=>
MDA-MB-231 MWXDfZRwfG:6aXPpeJkh[XO|YYm= MkTxO|IhcHK| MUHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA4OiCqcoOgZpkh[WyjbXHyJIJtfWViYYPzZZktKEWFNUCgQUAxNjByN{ig{txONg>? NYHyO2pNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0PVI{OTdpPkK4OFkzOzF5PD;hQi=>
HEK293 NF\tPWhHfW6ldHnvckBie3OjeR?= NGfGRmszKGi{cx?= MkHUTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDGUGFINXSjZ3fl[EBZUUGSIDj1cotvd3ewIH;ybYdqdiliaX70[ZJi[3Srb36ge4l1cCCodXzsJIxmdme2aDD1cpRi\2enZDDjZZNx[XOnLUmg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDh[pRmeiB{IHjyd{BjgSCrbX31co9xemWlaYDpeIF1cW:wIHHzd4F6NCCHQ{WwJF0hOC5yM{Wg{txONg>? NIrJU|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OES5NlMyPyd-Mki0PVI{OTd:L3G+
MDA-MB-231 NFW3VZFCdnSrdIXtc5Ih[XO|YYm= NHfBNlE{OCCvZz;r[y=> NIriOIwzPCCmYYnz M{ntTWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNieHXuc4dz[W[2ZXSgbY4hSmGuYj;jJHNEUURibX;1d4Uh[XO|ZYPz[YQh[XNidIXtc5Ih\3Kxd4ToJIlvcGmkaYTpc44h[XRiM{CgcYcwc2diYXTtbY5qe3SncnXkJJZq[SCxcnHsJIdifmGpZTDmc5IhOjRiZHH5dy=> MmfQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2OUKzNVcoRjJ6NEmyN|E4RC:jPh?=
MDA-MB-231 MljxSpVv[3Srb36gZZN{[Xl? MWqyJIhzew>? MXLJcoR2[3Srb36gc4YhcW62cnHj[YxtfWyjcjDjTWFROSCmZXfyZYRifGmxbjDpckBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDJiaILzMEBKSzVyIE2gNE4xODB2IN88UU4> Ml33QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByOUG2NFAoRjNyMEmxOlAxRC:jPh?=
MDA-MB-231 NITDe4RCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= Moe4O|IhcHK| NUjnVWVvSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCDbHHtZZIh[my3ZTDhd5NigSxiSVO1NEA:KDBwMEC3PEDPxE1w NVLHbWRnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwPVE3ODBpPkOwNFkyPjByPD;hQi=>
HEK293 M3;CdGZ2dmO2aX;uJIF{e2G7 M37UN|IhcHK| NHy1XG1KdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJGZNSUdvdHHn[4VlKFiLQWCgLJVvc26xd36gc5Jq\2mwKTDpcpRmemGldHnvckB4cXSqIH\1cIwhdGWwZ4ToJJVvfGGpZ3XkJINie3Cjc3WtPUBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzJIFnfGW{IEKgbJJ{KGK7IHntcZVvd3C{ZXPpdIl1[XSrb36gZZN{[XluIFnDOVAhRSByLkCzOUDPxE1w MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB7MU[wNEc,OzByOUG2NFA9N2F-
SKOV3 MkjzRZBweHSxc3nzJIF{e2G7 NWTFSVFZPDhiaILz NFLwUHVKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIGPLU3Y{KGOnbHzzJIF{e2W|c3XkJINie3Cjc3WtN{Bi[3SrdnH0bY9vKGGodHXyJFQ5KGi{czDifUBKdmO3Q4n0[UBUOyCuaY\lMYNmdGxiYX7hcJl{cXNuIFXDOVAhRSByLkCwNUDPxE1w M3G5VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzMEm1N|g3Lz5|MUC5OVM5PjxxYU6=
SKOV3 MlrtRZBweHSxc3nzJIF{e2G7 NELXfFQzPCCqcoO= NWLmV2o4UW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDTT29XOyClZXzsd{Bie3Onc4Pl[EBk[XOyYYPlMVMh[WO2aY\heIlwdiCjZoTldkAzPCCqcoOgZpkhUW6ldVP5eIUhWzNibHn2[U1k\WyuIHHuZYx6e2m|LDDFR|UxKD1iMD6wNFMh|ryPLh?= M3LsfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzMEm1N|g3Lz5|MUC5OVM5PjxxYU6=
BL21(DE3) MorDSpVv[3Srb36gZZN{[Xl? NYPDT2F4OiCqcoO= NWfMXW1UTGm|cHzhZ4Vu\W62IH;mJIJqd3SrbonsZZRm\CCDVmDGJIZzd21iTj30[ZJucW6jbDDIbZMhfGGpZ3XkJJJm[2:vYnnuZY51KGi3bXHuJHhKSVBvQlnSN{Bld22jaX6gLFI2OyC2bzCzOFchemW|aXT1[ZMqKGW6cILld5Nm\CCrbjDFd4Np\XKrY3jpZUBkd2yrIFLMNlEpTEV|KTDj[YxteyCrbnP1ZoF1\WRiZn;yJFIhcHK|IHL5JGRGVE[LQTygTWM2OCB;IECuNFQ5KM7:TT6= M4HjV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzMEm1N|g3Lz5|MUC5OVM5PjxxYU6=
BL21(DE3) M1jqXmZ2dmO2aX;uJIF{e2G7 MkTMPEBpenN? MojZSIl{eGyjY3Xt[Y51KG:oIHLpc5RqdnmuYYTl[EBCXlCIIH\yc40hVi22ZYLtbY5idCCKaYOgeIFo\2WmIILlZ49u[mmwYX70JIh2dWGwIGjJRXAuSkmUMzDkc41icW5iKEK1N{B1dyB|NEegdoV{cWS3ZYOpJIV5eHKnc4Pl[EBqdiCHc3Po[ZJq[2irYTDjc4xqKEKOMkGoSGU{MSClZXzsd{BqdmO3YnH0[YQh\m:{IEigbJJ{KGK7IFTFUGZKSSxiSVO1NEA:KDBwMEWzJO69VS5? M3Xtc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzMEm1N|g3Lz5|MUC5OVM5PjxxYU6=
A549 NHfVSYpHfW6ldHnvckBie3OjeR?= MYCxJJVO MX2zJIhzew>? NWDvNGJGUW6mdXP0bY9vKG:oIHPJRXAzKGSnZ4Lh[IF1cW:wIHnuJIh2dWGwIFG1OFkh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPJRXAzKHC{b4TlbY4hdGW4ZXygZZQhOSC3TTDpcoN2[mG2ZXSg[o9zKDNiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= NHrSR|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUW1NFE2PSd-M{G1OVAyPTV:L3G+
SK-MEL-28 NYLYXZpiTnWwY4Tpc44h[XO|YYm= NEPQcYcyKHWP MXizJIhzew>? MnHqTY5lfWO2aX;uJI9nKGOLQWCxJIRm\3KjZHH0bY9vKGmwIHj1cYFvKFONLV3FUE0zQCClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ2lCWDFicILveIVqdiCuZY\lcEBifCBzIIXNJIlv[3WkYYTl[EBnd3JiMzDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NUDsb3dbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G1OVAyPTVpPkOxOVUxOTV3PD;hQi=>
SK-MEL-28 NEDQNVJHfW6ldHnvckBie3OjeR?= NEnEeFQyKHWP NGLkR2g{KGi{cx?= NHXDeZlKdmS3Y4Tpc44hd2ZiY1nBVFIh\GWpcnHkZZRqd25iaX6gbJVu[W5iU1utUWVNNTJ6IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBkUUGSMjDwdo91\WmwIHzleoVtKGG2IEGgeW0hcW6ldXLheIVlKG[xcjCzJIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> MoXGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF3NUCxOVUoRjNzNUWwNVU2RC:jPh?=
HEK293T MojMSpVv[3Srb36gZZN{[Xl? Mk\KNVAhfU1? Mm[2OkBpenN? MonWR493[WynboSgZolv\GmwZzDh[oZqdmm2eTD0c{BJSS2ESWKzJIRwdWGrbjDv[kBZUUGSIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJGhGUzJ7M2SgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4h[mGwZDDpcpRmdnOrdImgZZQhOTBidV2gbY5kfWKjdHXkJIZweiB4IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTV3MEG1OUc,OzF3NUCxOVU9N2F-
A549 MWLGeY5kfGmxbjDhd5NigQ>? NEHLSoIyKHWP MXSzJIhzew>? MVXJcoR2[3Srb36gc4Yh[0mDUEGg[IVoemGmYYTpc44hcW5iaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[0mDUEGgdJJwfGWrbjDs[ZZmdCCjdDCxJJVOKGmwY4XiZZRm\CCob4KgN{BpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTV3MEG1OUc,OzF3NUCxOVU9N2F-
Assay
Methods Test Index PMID
Western blot cIAP1 / cIAP2 / XIAP / surivivin 27737687
Growth inhibition assay Cell viability 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]

  • 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

溶解度(25°C)

体外

* 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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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

请输入您的姓名
请输入您的邮箱地址 请输入一个有效的邮箱地址
请写点东西给我们
Tags: buy LCL161 | LCL161 supplier | purchase LCL161 | LCL161 cost | LCL161 manufacturer | order LCL161 | LCL161 distributor