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
RMB 3883.15 现货
RMB 8176.93 现货
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客户使用Selleck生产的LCL161发表文献21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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LOX NGWyNoNHfW6ldHnvckBie3OjeR?= NWnWTXp7QCCqcoO= M4PXb3BwfGWwdHnheIlwdiCxZjDjc45ifHWvdX3hZk1qdmS3Y3XkJINie3Cjc3WgN{84KGGldHn2ZZRqd25iaX6gbJVu[W5iTF;YJINmdGy|IIjlco9oemGodHXkJIlvKG2xdYPlJIFnfGW{IEigbJJ{KGK7IH\seY9z\XOlZX7j[UBie3OjeR?= M1zvXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEizO|gzLz5{NEC4N|c5OjxxYU6=
MDA-MB-231 NWT1[5dHTnWwY4Tpc44h[XO|YYm= MXOyMlUhfG9iMUCgeW0> NF\JOFYyQSCqcoO= MorhRolv\GmwZzDh[oZqdmm2eTD0c{BkUUGSMTDCTXI{KGSxbXHpckBqdiCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIGTOSoFteGijIHzleoVtKGG2IEKuOUB1dyBzMDD1UUBi\nSncjCxPUBpenNiYomgSWxKW0F? NG\XTpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4N|c5Oid-MkSwPFM4QDJ:L3G+
BxPC3 M2j0O2Z2dmO2aX;uJIF{e2G7 Mn;jN{4{KHWP M{PB[FUh\GG7cx?= NXL2SYpTWG:2ZX70bYF1cW:wIH;mJINwdmG2dX31cYFjNWmwZIXj[YQh[3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSniSQ{OgZ4VtdHNiYYSgN{4{KHWPIHHmeIVzKDViZHH5d{BjgSCPVGOgZZN{[Xl? M3POWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEizO|gzLz5{NEC4N|c5OjxxYU6=
HCT15 Mn;HSpVv[3Srb36gZZN{[Xl? Mn;HN{4{KHWP NEG0R2g2KGSjeYO= MmLNVI91\W62aXH0bY9vKG:oIHPvcoF1fW23bXHiMYlv\HWlZXSgZ5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTViY3XscJMh[XRiMz6zJJVOKGGodHXyJFUh\GG7czDifUBOXFNiYYPzZZk> Mn3oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEO3PFIoRjJ2MEizO|gzRC:jPh?=
SW620 NH[0W4xHfW6ldHnvckBie3OjeR?= M{P0WVEvOSC3TR?= MlTQOUBl[Xm| M1;GeHBwfGWwdHnheIlwdiCxZjDjc45ifHWvdX3hZk1qdmS3Y3XkJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNYPjJyIHPlcIx{KGG2IEGuNUB2VSCjZoTldkA2KGSjeYOgZpkhVVSVIHHzd4F6 MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB6M{e4Nkc,OjRyOEO3PFI9N2F-
SW620 MV7GeY5kfGmxbjDhd5NigQ>? MWezMlMhfU1? M3jDVVUh\GG7cx?= NEjRcZpRd3SnboTpZZRqd25ib3[gZ49v[XS3bYXtZYIucW6mdXPl[EBkgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUXzZ{MDDj[YxteyCjdDCzMlMhfU1iYX\0[ZIhPSCmYYnzJIJ6KE2WUzDhd5NigQ>? NW[2bZh2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFM4QDJpPkK0NFg{Pzh{PD;hQi=>
LOX MYjGeY5kfGmxbjDhd5NigQ>? MoO3N{4{KHWP NEXLdG4{KGSjeYO= Mk\qVI91\W62aXH0bY9vKG:oIHPvcoF1fW23bXHiMYlv\HWlZXSgZ5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUG9ZKGOnbHzzJIF1KDNwMzD1UUBi\nSncjCzJIRigXNiYomgUXRUKGG|c3H5 NIrlc|E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4N|c5Oid-MkSwPFM4QDJ:L3G+
LS180 M4WzNWZ2dmO2aX;uJIF{e2G7 M4S2e|MvOyC3TR?= NHTNNm42KGSjeYO= MWjQc5RmdnSrYYTpc44hd2ZiY3;uZZR2dXWvYXKtbY5lfWOnZDDjfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMV|E5OCClZXzsd{BifCB|LkOgeW0h[W[2ZYKgOUBl[Xm|IHL5JG1VWyCjc4PhfS=> NWm5W|VyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFM4QDJpPkK0NFg{Pzh{PD;hQi=>
H460 NEnFUZZHfW6ldHnvckBie3OjeR?= MonzN{4{KHWP MWS1JIRigXN? M2nWU3BwfGWwdHnheIlwdiCxZjDjc45ifHWvdX3hZk1qdmS3Y3XkJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGg1PjBiY3XscJMh[XRiMz6zJJVOKGGodHXyJFUh\GG7czDifUBOXFNiYYPzZZk> MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB6M{e4Nkc,OjRyOEO3PFI9N2F-
LOX MUDGeY5kfGmxbjDhd5NigQ>? M2LtT|ExOCCvZz;r[y=> M1;4RVghcHK| MljuVIxie22jIHPvcoNmdnS{YYTpc44hcW5iboXk[UBud3W|ZTD4[Y5w\3KjZoTl[EB4cXSqIHj1cYFvKEyRWDDj[YxteyCjdDCxNFAhdWdxa3esJJBwKG2nYYP1doVlKGG2IEigbJJ{NCCFcDC9JFMvOyEQvF2u M3rpOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEmzPVQxLz5{NEC5N|k1ODxxYU6=
SW620 NF\Pe5lHfW6ldHnvckBie3OjeR?= NVXRc|J4PSCmYYnz NH7MXnRKdmS3Y4Tpc44hd2Zic3Xud4l1cXqjdHnvckBw\iCqdX3hckBUXzZ{MDDj[YxteyC2bzDjc45ifHWvdX3hZk1qdmS3Y3XkJIFxd3C2b4Ppd{Bie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUBi\nSncjC1JIRigXNiYomgUXRUKGG|c3H5MEBGSzlyIE2gOk43PiEQvF2u NV7mWllnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPVM6PDBpPkK0NFk{QTRyPD;hQi=>
LOX MV3GeY5kfGmxbjDhd5NigQ>? M3rsU|ExOCCvZz;r[y=> MlTpPEBpenN? MofySJJ2\yC3cIThb4UhcW5idIXtc5Ihd2ZiboXk[UBud3W|ZTD4[Y5w\3KjZoTl[EB4cXSqIHj1cYFvKEyRWDDj[YxteyCjdDCxNFAhdWdxa3esJJBwKG2nYYP1doVlKGG2IEigbJJ{NCCGcoXnJJVxfGGtZTC9JFE5NjRizszNMi=> M3X2V|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEmzPVQxLz5{NEC5N|k1ODxxYU6=
SW620 NF;FT25HfW6ldHnvckBie3OjeR?= MlrmNk42KHWP MoKzOUBl[Xm| M4LPZ2lv\HWldHnvckBw\iC|ZX7zbZRqgmG2aX;uJI9nKGi3bXHuJHNYPjJyIHPlcIx{KHSxIHPvcoF1fW23bXHiMYlv\HWlZXSgZZBweHSxc3nzJIF{e2W|c3XkJIF{KGOnbHygeoli[mmuaYT5JIF1KDJwNTD1UUBi\nSncjC1JIRigXNiYomgUXRUKGG|c3H5 MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB7M{m0NEc,OjRyOUO5OFA9N2F-
LOX NV;0TJdUTnWwY4Tpc44h[XO|YYm= Ml3KNVAxKG2pL3vn NUO2PWVCQCCqcoO= MWfJckB3cX[xIHnubIljcXSrb36gc4YhYEmDUDDCTXIzKGSxbXHpckBqdiCqdX3hckBNV1hiY3XscJMhgGWwb3fyZYZ1\WRiaX6gcpVl\SCvb4Xz[UBie3Onc4Pl[EBieyCyb4TlcpRq[XSrb36gc4Yh[2:wYYT1cZVu[WJvaX7keYNm\CClYYPwZZNmKDNxNzDhZ5Rqfmm2eTDheEAyODBibXevb4ctKHCxIHHmeIVzKDhiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= M3O5RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEmzPVQxLz5{NEC5N|k1ODxxYU6=
LOX NFHpc|lHfW6ldHnvckBie3OjeR?= NXfB[YlTOTByIH3nM4to MWO4JIhzew>? NU\QcFI2UW5idnn2c{BqdmirYnn0bY9vKG:oIGjJRXAhSkmUMjDkc41icW5iaX6gbJVu[W5iTF;YJINmdGy|IIjlco9oemGodHXkJIlvKG63ZHWgcY92e2ViYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4h[2G|cHHz[UA{NzdiYXP0bZZqfHliYYSgNVAxKG2pL3vnMEBxdyCjZoTldkA5KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB7M{m0NEc,OjRyOUO5OFA9N2F-
MDA-MB-231 Ml\HSpVv[3Srb36gZZN{[Xl? NV3yO4l6OC5|NzD0c{A{NjNidV2= NFzIV3gyQSCqcoO= MlmwTY5pcWKrdHnvckBw\iClSVHQNU8zKGmwIHj1cYFvKE2GQT3NRk0zOzFiY3XscJMh[XO|ZYPz[YQh[XNiaX7keYN1cW:wIH;mJHRPTmGucHjhJIxmfmWuIHH0JFAvOzdidH:gN{4{KHWPIHHmeIVzKDF7IHjyd{BjgSCHTFnTRS=> NUXaVIlsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPVM6PDBpPkK0NFk{QTRyPD;hQi=>
CHL1 NXzX[2J1TnWwY4Tpc44h[XO|YYm= MnrCNE41KHSxIEGwJJVO MXSyPEBpenN? NGTucGFKdmirYnn0bY9vKG:oIHPJRXAyKGmwIHj1cYFvKEOKTEGgZ4VtdHNiYYSgNE41KHSxIEGwJJVOKGGodHXyJFI5KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NGSxUFc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC5N|k1OCd-MkSwPVM6PDB:L3G+
SKMES1 M17FUGZ2dmO2aX;uJIF{e2G7 MY[yMlUhfU1? NHnTNGI2KGSjeYO= NX7mdYxLWG:2ZX70bYF1cW:wIH;mJINwdmG2dX31cYFjNWmwZIXj[YQh[XCxcITvd4l{KGmwIHj1cYFvKFONTVXTNUBk\WyuczDheEAzNjVidV2gZYZ1\XJiNTDkZZl{KGK7IF3UV{Bie3OjeR?= M1nXS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEmzPVQxLz5{NEC5N|k1ODxxYU6=
Capan1 MkHGSpVv[3Srb36gZZN{[Xl? MUiyMlUhfU1? M{\OOFUh\GG7cx?= MnTMVI91\W62aXH0bY9vKG:oIHPvcoF1fW23bXHiMYlv\HWlZXSgZZBweHSxc3nzJIlvKGi3bXHuJGNieGGwMTDj[YxteyCjdDCyMlUhfU1iYX\0[ZIhPSCmYYnzJIJ6KE2WUzDhd5NigQ>? NX:5enlqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPVM6PDBpPkK0NFk{QTRyPD;hQi=>
AGS NIH2SopHfW6ldHnvckBie3OjeR?= MYCyMlUhfU1? MmXPOUBl[Xm| M1fyR2lv\HWldHnvckBw\iC|ZX7zbZRqgmG2aX;uJI9nKGi3bXHuJGFIWyClZXzsd{B1dyClb37heJVufW2jYj3pcoR2[2WmIHHwc5B1d3OrczDhd5Nme3OnZDDhd{Bk\WyuII\pZYJqdGm2eTDheEAzNjVidV2gZYZ1\XJiNTDkZZl{KGK7IF3UV{Bie3OjeR?= NGfVeW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC5N|k1OCd-MkSwPVM6PDB:L3G+
U118MG MVrGeY5kfGmxbjDhd5NigQ>? MUiyMlUhfU1? NUW4OlZnPSCmYYnz MXTQc5RmdnSrYYTpc44hd2ZiY3;uZZR2dXWvYXKtbY5lfWOnZDDhdI9xfG:|aYOgbY4hcHWvYX6gWVEyQE2JIHPlcIx{KGG2IEKuOUB2VSCjZoTldkA2KGSjeYOgZpkhVVSVIHHzd4F6 MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB7M{m0NEc,OjRyOUO5OFA9N2F-
PC3 MY\GeY5kfGmxbjDhd5NigQ>? NXnEfHFPOi53IIXN Mm\kOUBl[Xm| NWrudVhOUW6mdXP0bY9vKG:oIIPlcpNqfGm8YYTpc44hd2ZiaIXtZY4hWEN|IHPlcIx{KHSxIHPvcoF1fW23bXHiMYlv\HWlZXSgZZBweHSxc3nzJIF{e2W|c3XkJIF{KGOnbHygeoli[mmuaYT5JIF1KDJwNTD1UUBi\nSncjC1JIRigXNiYomgUXRUKGG|c3H5 MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB7M{m0NEc,OjRyOUO5OFA9N2F-
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SK-MEL-28 NHnuOVNHfW6ldHnvckBie3OjeR?= Mly0NUB2VQ>? MYOzJIhzew>? NXnNb5RzUW6mdXP0bY9vKG:oIHPJRXAyKGSnZ4Lh[IF1cW:wIHnuJIh2dWGwIGPLMW1GVC1{ODDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[0mDUEGgdJJwfGWrbjDs[ZZmdCCjdDCxJJVOKGmwY4XiZZRm\CCob4KgN{BpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ NWXiWVVORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G1OVAyPTVpPkOxOVUxOTV3PD;hQi=>
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HEK293T MlTjSpVv[3Srb36gZZN{[Xl? MWixNEB2VQ>? MljiOkBpenN? Ml;KR493[WynboSgZolv\GmwZzDh[oZqdmm2eTD0c{BJSS2ESWKzJIRwdWGrbjDv[kBZUUGSIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJGhGUzJ7M2SgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4h[mGwZDDpcpRmdnOrdImgZZQhOTBidV2gbY5kfWKjdHXkJIZweiB4IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= M3jOWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUWwNVU2Lz5|MUW1NFE2PTxxYU6=
A549 MkfBSpVv[3Srb36gZZN{[Xl? MXexJJVO MmOxN{BpenN? NVvIbIZFUW6mdXP0bY9vKG:oIHPJRXAyKGSnZ4Lh[IF1cW:wIHnuJIh2dWGwIFG1OFkh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPJRXAyKHC{b4TlbY4hdGW4ZXygZZQhOSC3TTDpcoN2[mG2ZXSg[o9zKDNiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTV3MEG1OUc,OzF3NUCxOVU9N2F-

... 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
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、MSDS / 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、MSDS / 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

IAP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID