Lenalidomide (CC-5013)

For research use only. Not for use in humans.

目录号:S1029 中文名称:来那度胺

Lenalidomide (CC-5013) Chemical Structure

CAS No. 191732-72-6

Lenalidomide (CC-5013)是一种TNF-α分泌抑制剂,在PBMCs中IC50为13 nM。Lenalidomide (CC-5013) 是 ubiquitin E3 ligase cereblon (CRBN) 的配体,它通过CRBN-CRL4泛素连接酶引起两个淋巴样转录因子IKZF1和IKZF3的选择性泛素化和降解。Lenalidomide 可促进 cleaved caspase-3 的表达、抑制 VEGF 的表达并诱导凋亡。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1557.33 现货
RMB 573.3 现货
RMB 1190.39 现货
RMB 3333.33 现货
RMB 4681.34 现货
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客户使用Selleck生产的Lenalidomide (CC-5013)发表文献122篇:

产品安全说明书

E3 ligase Ligand抑制剂选择性比较

生物活性

产品描述 Lenalidomide (CC-5013)是一种TNF-α分泌抑制剂,在PBMCs中IC50为13 nM。Lenalidomide (CC-5013) 是 ubiquitin E3 ligase cereblon (CRBN) 的配体,它通过CRBN-CRL4泛素连接酶引起两个淋巴样转录因子IKZF1和IKZF3的选择性泛素化和降解。Lenalidomide 可促进 cleaved caspase-3 的表达、抑制 VEGF 的表达并诱导凋亡。
靶点
CRBN [3]
()
VEGF [1]
()
TNF-α [1]
(PBMCs)
13 nM
体外研究

CC-5013强诱导IL-2和sIL-2R产量。CC-5013作用于T细胞,诱导CD28的酪氨酸磷酸化,随后下调NF-κB的激活。[2] Lenalidomide和Pomalidomide作用于表达与Thalidomide结合野生型CRBN的,而不是Thalidomide结合缺陷型CRBN(YW/AA)的HEK293 T细胞,抑制CRBN自体泛素化。KMS12多发性骨髓瘤细胞中,CRBN野生型蛋白而不是CRBN(YW/AA) 突变型蛋白的过表达, 放大Pomalidomide调节的c-myc和IRF4表达降低和p21(WAF-1) 表达增高。H929 多发性骨髓瘤细胞系中长期抗Lenalidomide 的选择性与CRBN降低相关,然而抗Pomalidomide和 Lenalidomide的DF15R多发性骨髓瘤 中, 检测不到CRBN蛋白。[3] Lenalidomide通过下调肿瘤细胞抑制性分子表达而抑制缺陷发生。Lenalidomide防止肿瘤诱导的T细胞裂解功能障碍发生。Lenalidomide 作用于T细胞,抑制慢性淋巴细胞性白血病(CLL)细胞诱导的T细胞肌动蛋白突触功能受损, 且下调CLL抑制配体及其他受体的表达。Lenalidomide 作用于FL, DLBCL, HL, MM, SCC,和 OC,抑制肿瘤诱导的免疫抑制,且作用于所有检测的肿瘤细胞时,下调免疫抑制配体表达。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LB771-HNC NF:5OVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3:xOWlEPTB;Mj6xOVA{QCEQvF2= M3\4flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFg1QC9pPmPBUmdGWjxxYU6=
L-363 M{jIdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWToOYoxUUN3ME2yMlkzOjF{IN88US=> MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly4OFgwLz6VQV7HSXI9N2F-
JAR MoHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUWwRohUUUN3ME2yMlk4ODBzIN88US=> MmeyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPFQ5Nyd-U1HOS2VTRC:jPh?=
EoL-1-cell NVzxVHY2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV2wXoRtUUN3ME20MlExPTF3IN88US=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly4OFgwLz6VQV7HSXI9N2F-
BT-549 NYrwO4RVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jiXWlEPTB;Nj6yNVg1QSEQvF2= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly4OFgwLz6VQV7HSXI9N2F-
SK-NEP-1 NHn0bGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHiOlNKSzVyPUeuPFk2OTJizszN NUTrd3MxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQDR6Lze+V2FPT0WUPD;hQi=>
BV-173 M1:5PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1v4XmlEPTB;OD62O|U5PSEQvF2= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly4OFgwLz6VQV7HSXI9N2F-
HMV-II MlnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTDTpFOUUN3ME2xNE4xOTd{IN88US=> M2rSZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFg1QC9pPmPBUmdGWjxxYU6=
HCC1806 NVfIZ|VNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTxTJhKSzVyPUGxMlQ1PjdizszN NVXBOY02RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQDR6Lze+V2FPT0WUPD;hQi=>
KASUMI-1 NH\YSFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnThTWM2OD1zMT61O|Eh|ryP NFvFS4I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw5PDhxJ{7TRW5ITVJ:L3G+
SK-MEL-28 M2nJVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTFzLkm3OlQh|ryP Mo\BQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPFQ5Nyd-U1HOS2VTRC:jPh?=
RPMI-8226 Ml\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTlTWM2OD1zMj62NlQyKM7:TR?= NXfCeHBvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQDR6Lze+V2FPT0WUPD;hQi=>
T47D MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rDZmlEPTB;MUOuNlA6QSEQvF2= NIe4cVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw5PDhxJ{7TRW5ITVJ:L3G+
HOP-62 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTF|LkS4JO69VQ>? M{TITlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFg1QC9pPmPBUmdGWjxxYU6=
A2058 NVrXXZhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLoU4p7UUN3ME2xN{45OTl7IN88US=> M2DncFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFg1QC9pPmPBUmdGWjxxYU6=
SW620 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWSwXmFTUUN3ME2xOE4zPDd|IN88US=> NX3yT5JuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQDR6Lze+V2FPT0WUPD;hQi=>
LCLC-103H MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHlSWpKSzVyPUG0MlQ5QTJizszN M4WxZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFg1QC9pPmPBUmdGWjxxYU6=
HAL-01 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHKwdXFKSzVyPUG0MlU4QTZizszN MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly4OFgwLz6VQV7HSXI9N2F-
PANC-08-13 NX:1c21kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTF2LkmxNFgh|ryP NYWzNlF5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQDR6Lze+V2FPT0WUPD;hQi=>
COLO-684 M1e5Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\PPWlEPTB;MUWuN|k4QSEQvF2= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly4OFgwLz6VQV7HSXI9N2F-
DEL MnXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTF3LkS5PUDPxE1? M{f5S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFg1QC9pPmPBUmdGWjxxYU6=
K5 NGXJ[Y5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTF4LkG0PFYh|ryP M4HFVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFg1QC9pPmPBUmdGWjxxYU6=
SK-MEL-24 M3LCSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3JTWM2OD1zNj60OlUzKM7:TR?= M{DyNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFg1QC9pPmPBUmdGWjxxYU6=
ACN NI\6XplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTF4LkWyPVch|ryP MoDwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPFQ5Nyd-U1HOS2VTRC:jPh?=
H9 MnrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HUOGlEPTB;MU[uOlI3KM7:TR?= NXPPbHZNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQDR6Lze+V2FPT0WUPD;hQi=>
EM-2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHm2cmhKSzVyPUG3MlE1OyEQvF2= NHHDTXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw5PDhxJ{7TRW5ITVJ:L3G+
HSC-4 NUfTdIE3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTF5Lk[2NFEh|ryP MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly4OFgwLz6VQV7HSXI9N2F-
IGROV-1 NU\YV41FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHiSW9KSzVyPUG3Mlc5OyEQvF2= M4TVVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFg1QC9pPmPBUmdGWjxxYU6=
TE-1 M{\JfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTF5Lkm5Olgh|ryP MlS2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPFQ5Nyd-U1HOS2VTRC:jPh?=
LN-405 MmPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TzeGlEPTB;MUmuPVA4PiEQvF2= M2TSRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFg1QC9pPmPBUmdGWjxxYU6=
MSTO-211H M4TMbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LMTmlEPTB;MkCuN|U4OyEQvF2= NFzUZ3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw5PDhxJ{7TRW5ITVJ:L3G+
MOLT-4 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TvUmlEPTB;MkCuOVc2QSEQvF2= MkjnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPFQ5Nyd-U1HOS2VTRC:jPh?=
RS4-11 M4r0OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7zTJJKSzVyPUKyMlE2PjNizszN NWfPXlM4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQDR6Lze+V2FPT0WUPD;hQi=>
ES3 MnPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIr6VYZKSzVyPUKyMlY6PjNizszN NV7sfI1ZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQDR6Lze+V2FPT0WUPD;hQi=>
SBC-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrHd3BoUUN3ME2yN{45Pjl4IN88US=> MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly4OFgwLz6VQV7HSXI9N2F-
CTV-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7YTWM2OD1{NT6wNVQ6KM7:TR?= NF7kT5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw5PDhxJ{7TRW5ITVJ:L3G+
HuP-T3 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nId2lEPTB;MkWuOFAxQSEQvF2= M13INVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFg1QC9pPmPBUmdGWjxxYU6=
HCC2218 MknoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWftbZM{UUN3ME2yOU42PDB5IN88US=> MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly4OFgwLz6VQV7HSXI9N2F-
HDLM-2 M1m0cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY[4NXlSUUN3ME2yPE4zODJ4IN88US=> MlPyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPFQ5Nyd-U1HOS2VTRC:jPh?=
ABC-1 M{X0SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIS4dmxKSzVyPUK5MlY6PzRizszN M4PselxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFg1QC9pPmPBUmdGWjxxYU6=
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CD34+ progenitor cells M1jIdWZ2dmO2aX;uJIF{e2G7 M4X4PVE1KGSjeYO= M36xbWRm[3KnYYPlJIlvKGW{eYTodo9q\CCmaX\m[ZJmdnSrYYTpc44hd2ZiQ1SzOEsheHKxZ3XubZRweiClZXzsd{Bnem:vIH35[Yxw\Hm|cHzhd5Rq[yC|eX7kdo9u\SCmZXyoOZEqKHCjdHnlcpQh[XO|ZYPz[YQh[XNiQ1SzOkBmgHC{ZYPzbY9vKGGodHXyJFE1KGSjeYO= NVrBWpdkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1O|Y6OjRpPkG3OVc3QTJ2PD;hQi=>
CD34+ progenitor cells MYPGeY5kfGmxbjDhd5NigQ>? MXSxOEBl[Xm| NFztdHVF\WO{ZXHz[UBqdiCveXXsc4llKGSrZn\ldoVvfGmjdHnvckBw\iCFREO0L{Bxem:pZX7peI9zKGOnbHzzJIZzd21ibYnlcI9lgXOybHHzeIlkKHO7bnTyc41mKGSnbDi1dUkheGG2aXXueEBie3Onc4Pl[EBieyCFREOzJIV5eHKnc4Ppc44h[W[2ZYKgNVQh\GG7cx?= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV5NkmyOEc,OTd3N{[5NlQ9N2F-
CD34+ progenitor cells M2LPTWZ2dmO2aX;uJIF{e2G7 MkPENVQh\GG7cx?= NX3kRoh2TGWlcnXhd4UhcW5iZYL5eIhzd2mmIHTp[oZmemWwdHnheIlwdiCxZjDDSFM1MyCycn;n[Y5qfG:{IHPlcIx{KG[{b32gcZlmdG:meYPwcIF{fGmlIIP5coRzd22nIHTlcEg2eSlicHH0bYVvfCCjc4Pld5Nm\CCjczDncJlkd3Cqb4LpckBCKGW6cILld5Nqd25iYX\0[ZIhOTRiZHH5dy=> M2fmd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUe2PVI1Lz5zN{W3OlkzPDxxYU6=
CD34+ progenitor cells NWXMT41rT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mke1NVQh\GG7cx?= M1LKbmlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIH;mJGNFOzRtIIDyc4dmdmm2b4KgZ4VtdHNiZoLvcUBugWWub3T5d5Bt[XO2aXOgd5lv\HKxbXWg[IVtMDWzKTDwZZRq\W62IHHmeIVzKDF2IHThfZM> M1rmXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUe2PVI1Lz5zN{W3OlkzPDxxYU6=
CD34+ progenitor cells NHviWFNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH3IWYIyPCCmYYnz NF\GT4hIem:5dHigbY5pcWKrdHnvckBw\iCFREO0L{Bxem:pZX7peI9zKGOnbHzzJIZzd21ibn;uMYRmdCh3cTmgcZlmdG:meYPwcIF{fGmlIIP5coRzd22nIIDheIlmdnRiYX\0[ZIhOTRiZHH5dy=> MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV5NkmyOEc,OTd3N{[5NlQ9N2F-
DF15 Mn7HSpVv[3Srb36gZZN{[Xl? Moe0NE4yKHSxIEGwJJVO MUW1JIhzew>? M{T4[Wlv\HWldHnvckBw\iClZYLlZoxwdi2vZXTpZZRm\CCjaX;sc5Mh\GWpcnHkZZRqd25iaX6gbJVu[W5iRF[xOUBk\WyuczDheEAxNjFidH:gNVAhfU1iYX\0[ZIhPSCqcoOgZpkhcW2vdX7vZoxwfCCjbnHsfZNqew>? NVK3cYZnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0NlU4OjBpPkK4OFI2PzJyPD;hQi=>
OPM2 M1PvV2Z2dmO2aX;uJIF{e2G7 M1nWelAvOSC2bzCxNEB2VQ>? NIjudlU2KGi{cx?= NF3UXI1KdmS3Y4Tpc44hd2ZiY3Xy[YJtd25vbXXkbYF1\WRiYXnvcI9{KGSnZ4Lh[IF1cW:wIHnuJIh2dWGwIF;QUVIh[2WubIOgZZQhOC5zIITvJFExKHWPIHHmeIVzKDViaILzJIJ6KGmvbYXuc4Jtd3RiYX7hcJl{cXN? MnzuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2MkW3NlAoRjJ6NEK1O|IxRC:jPh?=
DF15 MULGeY5kfGmxbjDhd5NigQ>? MoLINE4yKHSxIEGwJJVO NU\2R4JEPSCqcoO= MoHiTY5lfWO2aX;uJI9nKGOncnXicI9vNW2nZHnheIVlKGmtYYLvd{Bl\We{YXTheIlwdiCrbjDoeY1idiCGRkG1JINmdGy|IHH0JFAvOSC2bzCxNEB2VSCjZoTldkA2KGi{czDifUBqdW23bn;icI91KGGwYXz5d4l{ NUnOVXpsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0NlU4OjBpPkK4OFI2PzJyPD;hQi=>
OPM2 M3vRSmZ2dmO2aX;uJIF{e2G7 MoPhNE4yKHSxIEGwJJVO NFqyWFI2KGi{cx?= MoXITY5lfWO2aX;uJI9nKGOncnXicI9vNW2nZHnheIVlKGmtYYLvd{Bl\We{YXTheIlwdiCrbjDoeY1idiCRUF2yJINmdGy|IHH0JFAvOSC2bzCxNEB2VSCjZoTldkA2KGi{czDifUBqdW23bn;icI91KGGwYXz5d4l{ MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR{NUeyNEc,Ojh2MkW3NlA9N2F-
EC9706 MoH1RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? Mn;uNVUxKHWpL33M NYDtflVCPDhiaILz MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEWFOUewOkBk\WyuczDheEAyPTBidXevcWwh[W[2ZYKgOFghcHK|IHL5JGNEUy16IHHzd4F6 M4LoUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{W3NFY3Lz5{OEe1O|A3PjxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
phospho-IKKβ / IKKβ ; 

PubMed: 22698399     


Western blot analysis of the indicated proteins following treatment of OCI-Ly10 cells with lenalidomide (10μM) for the indicated times. 

MDM2 / p-MDM2 / p-p53 / p53 ; 

PubMed: 22525275     


(a) Treatment with lenalidomide (Len) increases phosphorylation of ser46 and thr55 of p53. Namalwa cells were treated with lenalidomide at various concentrations for 48 hours, the cell lysates were prepared and analyzed by Western blotting with antibodies to MDM2, phospho-ser46 of p53, phospho-thr55 of p53 and total p53. (b) Treatment with lenalidomide increases phosphorylation of MDM2 at ser166 and ser186. Namalwa cells were treated with lenalidomide at various concentrations for 48 hours, the cell lysates were immunoprecipitated using anti-MDM2 antibody. The samples were separated by SDS PAGE and then Western blotted with either anti-MDM2 or antibodies specific to phospho-ser166, phospho-ser186, total phospho-serine or total phospho-threonine of MDM2 as indicated. 

22698399 22525275
Growth inhibition assay
Cell viability; 

PubMed: 22698399     


Viability (MTS assay) of ABC and GCB DLBCL cell lines treated with lenalidomide for 4 days. Error bars show the standard error of the mean (SEM) of triplicates.

22698399
体内研究 口服处理Lenalidomide,显著抑制bFGF诱导的血管生成,这种作用存在剂量依赖性。Lenalidomide 显著降低血管面积百分数,从对照组的5.16%降低到实验组的2.58(50 mg/kg剂量处理)和 1.69(250 mg/kg 剂量处理)。 Lenalidomide 显著降低全部MVL,从对照组的21.07降低到实验组的8.11(50 mg/kg剂量处理)和1.90(250 mg/kg剂量处理)。[5]

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)

激酶实验:

[1]

- 合并

Assay for inhibition of TNF synthesis by human PBMCs:

Human PBMCs from normal donors are obtained by Ficoll−Hypaque density centrifugation. Cells (106 cells/mL) are cultured in RPMI supplemented with 10 AB+ serum, 2 mM l-glutamine, 100 U/mL penicillin, and 100 μg/mL streptomycin. Lenalidomide is dissolved in DMSO at 20 mg/mL; further dilution is done with culture medium. The final DMSO concentration in all assays including the controls is 0.25%. Lenalidomide is added to cells 1 hour prior to the addition of LPS. PBMCs (106 cells/mL) are stimulated with 1 μg/mL of LPS from Salmonella minnesota R595. Cells, in triplicate, are incubated with LPS for 18−20 hours at 37 °C in 5% CO2. Supernatants are then harvested and assayed for cytokine levels. In some experiments, supernatants are kept frozen at −70 °C until use. Cell viability is assayed by Trypan blue exclusion dye method. The concentration of TNFα in the culture supernatants is determined by ELISA. Lenalidomide is assayed in a minimum of three separate experiments. Percent inhibition is determined as 100 × [1 − (cytokine(experimental)/cytokine(control))].
细胞实验: [3]
- 合并
  • Cell lines: 良性或恶性 B (CLL)细胞, RPMI8226 MM 细胞
  • Concentrations: 1 μM或5 nM
  • Incubation Time: 24小时
  • Method: 使用CellTracker Blue CMAC对良性或恶性B (CLL)细胞(2 × 106)进行染色, 然后使用2 μg/mL金黄色葡萄球菌超抗原(sAg) (SEA 和 SEB) 在37oC下进行脉冲处理30分钟。B细胞和等量T细胞(从原代共培养中纯化的)按200 × g转速离心5分钟,然后与CD8+ T 细胞在37oC下温育10分钟,或者与 CD3+ T细胞温育20分钟。使用细胞收集器使细胞转移到显微镜载玻片上,然后在室温下和3% 溶于PBS的甲醛混合15分钟。在完全培养基中加入终浓度为1 μM的Lenalidomide。对照组则使用DMSO处理细胞。
    (Only for Reference)
动物实验:[5]
- 合并
  • Animal Models: 携带HUVECs细胞的成年雄性Sprague–Dawley大鼠
  • Dosages: 50 mg/kg和250 mg/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 52 mg/mL (200.57 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+40%PEG 300+5%Tween80+ddH2O
10mg/mL

* 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 259.26
化学式

C13H13N3O3

CAS号 191732-72-6
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、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
NCT04903197 Not yet recruiting Drug: VAY736|Drug: lenalidomide Non-Hodgkin Lymphoma Diffuse Large B Cell Lymphoma Novartis Pharmaceuticals|Novartis September 30 2021 Phase 1
NCT04974216 Not yet recruiting Drug: Tafasitamab|Drug: Lenalidomide|Drug: Rituximab DLBCL The Lymphoma Academic Research Organisation September 15 2021 Phase 2
NCT04669171 Recruiting Biological: EO2463|Drug: lenalidomide|Biological: rituximab Follicular Lymphoma|Marginal Zone Lymphoma Enterome July 5 2021 Phase 1|Phase 2
NCT04796857 Recruiting Drug: PD-1 Antibody|Drug: Lenalidomide Non-GCB/ABC Diffuse Large B-Cell Lymphoma|High-grade B-cell Lymphoma|Follicular Lymphoma Grade IIIb|Transformed Lymphoma|EBV-Positive DLBCL Nos|ALK-Positive Anaplastic Large Cell Lymphoma Huiqiang Huang|Sun Yat-sen University March 31 2021 Phase 1|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

常见问题及建议解决方法

  • 问题 1:

    What is the formulation for mouse injection(i.p.)?

  • 回答:

    This paper has the information you need: http://link.springer.com/article/10.1208/s12248-012-9401-2. Add lenalidomide to the appropriate volume of sterile phosphate-buffered saline (PBS) containing 1% hydrochloric acid (HCl). the pH of this preparation was adjusted to 7.0–7.6 using sodium hydroxide and sterile filtered using a 0.22 μm Steriflip filter.

  • 问题 2:

    what is the procedure to resuspend this compound?

  • 回答:

    You can resuspend this compund by DMSO, the solubility is about 52 mg/mL (200.57 mM). For in vivo study, you can prepare the working solution with the vehicle of: 30% PEG400/0.5% Tween80/5% propylene glycol for oral administration.

E3 ligase Ligand Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID