Lenalidomide (CC-5013) 化学構造
分子量: 259.26

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製品説明

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    併用療法

製品の説明

生物活性

製品説明 Lenalidomide (CC-5013) は、13nMのIC50によるTNF-α分泌阻害剤です。
ターゲット

TNF-α

IC50

13 nM [1]

In vitro試験 Lenalidomide strongly induces IL-2 and sIL-2R production. Lenalidomide-induced tyrosine phosphorylation of CD28 on T cells is followed by a down-stream activation of NF-κB. [2] Lenalidomide and pomalidomide inhibits autoubiquitination of CRBN in HEK293 T cells expressing thalidomide-binding competent wild-type CRBN, but not thalidomide-binding defective CRBN(YW/AA). Overexpression of CRBN wild-type protein, but not CRBN(YW/AA) mutant protein, in KMS12 myeloma cells, amplifies pomalidomide-mediated reductions in c-myc and IRF4 expression and increases in p21(WAF-1) expression. Long-term selection for Lenalidomide resistance in H929 myeloma cell lines is accompanied by a reduction in CRBN, while in DF15R myeloma cells resistant to both pomalidomide and Lenalidomide, CRBN protein is undetectable. [3] Lenalidomide prevents induction of defects by down-regulating tumor cell inhibitory molecule expression. Lenalidomide prevents induction of tumor-induced T cell lytic synapse dysfunction. Lenalidomide treatment blocks CLL cell-induced T cell actin synapse dysfunction, mimicks antibody blockade, and down-regulates expression of CLL inhibitory ligands and their receptors on T cells. Lenalidomide treatment prevents tumor-induced immune suppression in FL, DLBCL, HL, MM, SCC, and OC and down-regulates immunosuppressive ligand expression on all tumor cells examined. CTL killing function significantly increases following antibody blockade of CLL inhibitory ligands or Lenalidomide treatment compared to control treatments. Treatment of autologous CLL-T cell co-cultures with Lenalidomide reverses impaired CD8+ T cell lytic synapse formation and granzyme B trafficking. [4]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
LB771-HNC MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDs[3VKSzVyPUKuNVUxOzhizszN MYjTRW5ITVJ?
L-363 M2HLfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXwVHFKSzVyPUKuPVIzOTJizszN M3PLWHNCVkeHUh?=
JAR NXXIRZJRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nabmlEPTB;Mj65O|AxOSEQvF2= NYPufmRzW0GQR1XS
EoL-1-cell MorlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPMWpg5UUN3ME20MlExPTF3IN88US=> MX\TRW5ITVJ?
BT-549 NIW4eHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH[xUWNKSzVyPU[uNlE5PDlizszN MXTTRW5ITVJ?
SK-NEP-1 NEHw[oNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;GbGlKSzVyPUeuPFk2OTJizszN M1LWSXNCVkeHUh?=
BV-173 NHzlOYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEezbnVKSzVyPUiuOlc2QDVizszN NHXQSGRUSU6JRWK=
HMV-II MnLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTFyLkCxO|Ih|ryP NUD0SJQzW0GQR1XS
HCC1806 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfBTWM2OD1zMT60OFY4KM7:TR?= M3LENHNCVkeHUh?=
KASUMI-1 NU\3N4pIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLWTWM2OD1zMT61O|Eh|ryP Mm\kV2FPT0WU
SK-MEL-28 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33GTmlEPTB;MUGuPVc3PCEQvF2= NU\QUlN7W0GQR1XS
RPMI-8226 MlHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jQcmlEPTB;MUKuOlI1OSEQvF2= NVPkbZVIW0GQR1XS
T47D MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXQ[nc1UUN3ME2xN{4zODl7IN88US=> MVfTRW5ITVJ?
HOP-62 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTF|LkS4JO69VQ>? NH;KSmtUSU6JRWK=
A2058 NHXKd4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTF|LkixPVkh|ryP NX3ZRYRWW0GQR1XS
SW620 NWG3dIp2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTF2LkK0O|Mh|ryP NWLHe49WW0GQR1XS
LCLC-103H MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFf4UJVKSzVyPUG0MlQ5QTJizszN NUjBRnNZW0GQR1XS
HAL-01 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTF2LkW3PVYh|ryP Mni0V2FPT0WU
PANC-08-13 M{XrVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXuXHNKSzVyPUG0MlkyODhizszN M1W4fHNCVkeHUh?=
COLO-684 NU\NRmx[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTmNVdKSzVyPUG1MlM6PzlizszN MVfTRW5ITVJ?
DEL MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nzTmlEPTB;MUWuOFk6KM7:TR?= M3fSR3NCVkeHUh?=
K5 NVm1W2NzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrVTWM2OD1zNj6xOFg3KM7:TR?= NFPRT5pUSU6JRWK=
SK-MEL-24 MmPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzrTWM2OD1zNj60OlUzKM7:TR?= MlvKV2FPT0WU
ACN NUTGb5RuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTF4LkWyPVch|ryP M{m2eXNCVkeHUh?=
H9 NXXXS3l7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\6bXlKSzVyPUG2MlYzPiEQvF2= M2rNXXNCVkeHUh?=
EM-2 NIfWOGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzYPIVKSzVyPUG3MlE1OyEQvF2= MkG5V2FPT0WU
HSC-4 NYq4VIlET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDhTWM2OD1zNz62OlAyKM7:TR?= NYPaWYVvW0GQR1XS
IGROV-1 NUfm[HdvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPweYNKSzVyPUG3Mlc5OyEQvF2= MkTnV2FPT0WU
TE-1 M3e1Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIW2WnRKSzVyPUG3Mlk6PjhizszN MV3TRW5ITVJ?
LN-405 MmrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{K2N2lEPTB;MUmuPVA4PiEQvF2= NVnWSohJW0GQR1XS
MSTO-211H MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{P3TGlEPTB;MkCuN|U4OyEQvF2= NXu4Um1oW0GQR1XS
MOLT-4 M2npb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTJyLkW3OVkh|ryP MkKzV2FPT0WU
RS4-11 M174dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDhXnhqUUN3ME2yNk4yPTZ|IN88US=> M4T0OXNCVkeHUh?=
ES3 M{n2UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LXeWlEPTB;MkKuOlk3OyEQvF2= MmXIV2FPT0WU
SBC-1 M2P1fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1qwdmlEPTB;MkOuPFY6PiEQvF2= MkOxV2FPT0WU
CTV-1 MoHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LJbmlEPTB;MkWuNFE1QSEQvF2= M2\FO3NCVkeHUh?=
HuP-T3 NGLuRYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;vRmlEPTB;MkWuOFAxQSEQvF2= MV7TRW5ITVJ?
HCC2218 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\GTWM2OD1{NT61OFA4KM7:TR?= NVjm[WJSW0GQR1XS
HDLM-2 MlrqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\yW5BKSzVyPUK4MlIxOjZizszN NEDJfWtUSU6JRWK=
ABC-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTJ7Lk[5O|Qh|ryP NFz4fo1USU6JRWK=
MV-4-11 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\XXmU{UUN3ME2yPU44OzF5IN88US=> NF;zR2VUSU6JRWK=
WM-115 NF;wdGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3q0bGlEPTB;M{CuN|A6QSEQvF2= M3HYXHNCVkeHUh?=
SW1990 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3xTWM2OD1|MD6zN{DPxE1? MVjTRW5ITVJ?
HCC70 MoTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHtTWM2OD1|MD63N|Q3KM7:TR?= Mnr2V2FPT0WU
KYSE-520 NGX0c3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PZXmlEPTB;M{CuPFg{QSEQvF2= NFzESJZUSU6JRWK=
JEG-3 M{PrXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LtSmlEPTB;M{GuNVYyPCEQvF2= M2LKT3NCVkeHUh?=
C8166 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvMRZFKSzVyPUOxMlIzPzRizszN M4j5VHNCVkeHUh?=
SK-OV-3 NXG5Tnd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTNzLk[3OVUh|ryP M4fqOnNCVkeHUh?=
NCI-H526 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTN{Lk[4N{DPxE1? NVTMXXFCW0GQR1XS
NKM-1 NF3jUG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\xSldHUUN3ME2zNk46PTZ6IN88US=> MVPTRW5ITVJ?
ECC10 MkX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3BSVUyUUN3ME2zOE44PDR|IN88US=> MUfTRW5ITVJ?
A2780 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTN3LkO2NFEh|ryP NWj1cVR3W0GQR1XS
KY821 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\mdmlEPTB;M{WuO|Y5OSEQvF2= NIX6ZVBUSU6JRWK=
MKN1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLz[ZpKSzVyPUO2MlIyOzdizszN MX7TRW5ITVJ?
EKVX M4LW[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnmTWM2OD1|Nz60NlEzKM7:TR?= NHOySGlUSU6JRWK=
EW-16 MmHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTN6LkO4PFUh|ryP M3HOXXNCVkeHUh?=
CTB-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHqTWM2OD1|OT63O|g6KM7:TR?= NIj2VWVUSU6JRWK=
COR-L105 NH;nVHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzJR3R5UUN3ME20NE41PzR4IN88US=> M2q1[nNCVkeHUh?=
NCI-SNU-5 NGLM[IxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mke2TWM2OD12MT6yNFY6KM7:TR?= MUTTRW5ITVJ?
Mewo MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfDZ5Y2UUN3ME20NU46QDdzIN88US=> NGDQSnpUSU6JRWK=
BCPAP NVX3XlIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jtZ2lEPTB;NEOuO|kyPyEQvF2= NWrmbI5lW0GQR1XS
KARPAS-45 M{THOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLnV4pKSzVyPUS0MlI4PzZizszN M{njfHNCVkeHUh?=
NCI-H1693 NVLPUVB4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\Xc2lEPTB;NE[uOlk5PiEQvF2= MlzIV2FPT0WU
H-EMC-SS MlPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofGTWM2OD12OD6zNlI1KM7:TR?= MmLtV2FPT0WU
697 NGDFfm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfPRYFyUUN3ME21NE4{PTR3IN88US=> M4nzOXNCVkeHUh?=
KP-N-YS MorBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfKbWJuUUN3ME21Nk4{OTR{IN88US=> MVTTRW5ITVJ?
NCI-H1304 NF3UWYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfMT2M6UUN3ME21Nk44ODJ2IN88US=> M3jiU3NCVkeHUh?=
NOS-1 MkHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLwW49CUUN3ME21Nk45PTV7IN88US=> NXKzNW9kW0GQR1XS
NCI-H2342 MlnUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTV|LkC1NFgh|ryP MWjTRW5ITVJ?
KYSE-270 NFHieJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETEcmtKSzVyPUWzMlY{PjRizszN NX74UHJzW0GQR1XS
LU-135 NG\ifmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTV3LkG4OVMh|ryP MYfTRW5ITVJ?
OE33 M2XqXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXJOGRKSzVyPUW1MlgyQCEQvF2= MVTTRW5ITVJ?
ML-2 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTV3Lkm0PFkh|ryP MXTTRW5ITVJ?
KMOE-2 NGi1VZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mme1TWM2OD13Nj6yPFk{KM7:TR?= MYrTRW5ITVJ?
Daoy MkL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTV4LkOyNFQh|ryP NYfJOFBPW0GQR1XS
KNS-62 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLtUHhXUUN3ME21O{4xOTR{IN88US=> MkLLV2FPT0WU
NBsusSR M17scWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULSeXNMUUN3ME21O{42PzB3IN88US=> NXO1Z|ZKW0GQR1XS
UACC-257 Mn7TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;4XWtKSzVyPUW4MlYzPjRizszN M3\mPHNCVkeHUh?=
LU-139 M1zWT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTV6LkiyOkDPxE1? MUXTRW5ITVJ?
CAL-85-1 M2rnO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{G0N2lEPTB;NUiuPFY1OyEQvF2= M3m0SXNCVkeHUh?=
NCI-H720 MnjyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTV6Lki5OFIh|ryP MVHTRW5ITVJ?
MLMA MoDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzrTWM2OD13OT6wPVEh|ryP M{Lxe3NCVkeHUh?=
A3-KAW M3\5S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXHTWM2OD13OT6yPFA6KM7:TR?= M4T4V3NCVkeHUh?=
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GCT MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLGdJpKSzVyPU[xMlA4QDZizszN M3TqWHNCVkeHUh?=
K-562 NFnGRXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljPTWM2OD14MT61N|M{KM7:TR?= MnvGV2FPT0WU
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NCI-H1993 M1rreGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTZ|LkSwOFMh|ryP NH72PWtUSU6JRWK=
NCI-H358 NGSxSFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjod4ZKSzVyPU[1MlAyOjFizszN MUTTRW5ITVJ?
NB6 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\WU2JKSzVyPU[1Mlk5QCEQvF2= M{fDSHNCVkeHUh?=
HCE-T NX35UFZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;BUGdKSzVyPU[3MlA4QThizszN MmLQV2FPT0WU
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HT-1376 M1POfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MneyTWM2OD14OT64N|E1KM7:TR?= NE\3fVNUSU6JRWK=
NEC8 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7JcpNKSzVyPUewMlEzPDNizszN NEXyNmtUSU6JRWK=
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NCI-H69 NHLQOWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmSzTWM2OD15NT63OlY{KM7:TR?= MnvmV2FPT0WU
NCI-H209 NIG4bXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHmWG5KSzVyPUe4MlYyPDdizszN MWPTRW5ITVJ?
CAL-33 NWT4fId[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTd6Lkm5N|kh|ryP MULTRW5ITVJ?
COLO-680N NVz6W4RxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTd7LkGwNFch|ryP NIXnOWVUSU6JRWK=
D-283MED NEPQRpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTd7LkixNkDPxE1? MkPGV2FPT0WU
ATN-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jzO2lEPTB;OEGuNVE5PyEQvF2= NWLrXXA6W0GQR1XS
NCI-N87 MorWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRThzLkeyPVYh|ryP M2HUTXNCVkeHUh?=
MHH-NB-11 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUWx[24zUUN3ME24NU45QDR7IN88US=> M33sZnNCVkeHUh?=
HEL NXTuV|B5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjYTWM2OD16Mj60NVM1KM7:TR?= M3fKS3NCVkeHUh?=
NB69 MnzpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTh|LkCwN|Mh|ryP MWrTRW5ITVJ?
MPP-89 MnjIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3Px[WlEPTB;OEOuNlU4PSEQvF2= MkjwV2FPT0WU
COLO-829 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXFbJM{UUN3ME24OU41QTF{IN88US=> MnXJV2FPT0WU
ONS-76 M4Dz[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTh3Lke5NFgh|ryP M{Hib3NCVkeHUh?=
EW-3 MonUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETNfIxKSzVyPUi2MlIxOzJizszN NFrQWnRUSU6JRWK=
EW-11 NEf1VIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDIbpRjUUN3ME24Ok41OzN4IN88US=> MWfTRW5ITVJ?
SW900 NVfzNWpUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Pl[WlEPTB;OEeuNlA2OyEQvF2= MYTTRW5ITVJ?
MOLT-13 NEHaOlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGewWW5KSzVyPUi3MlIzPDNizszN M{DEbXNCVkeHUh?=
HuP-T4 MmDPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17r[GlEPTB;OUGuNFQxPSEQvF2= NEjQVmdUSU6JRWK=
HCC1419 Ml6xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF:1VHhKSzVyPUmxMlY{PzRizszN MYPTRW5ITVJ?
CAL-72 M{e1N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\UTohKSzVyPUmyMlAzOTlizszN MUfTRW5ITVJ?
Mo-T MkPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnFPGxjUUN3ME25Nk44Pjl5IN88US=> MUnTRW5ITVJ?
OC-314 NH[0ZWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTiTWM2OD17Mj64PFIyKM7:TR?= MV\TRW5ITVJ?
BHT-101 NX;pRpc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTl|LkGg{txO M4XxNnNCVkeHUh?=
EW-18 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfTclZDUUN3ME25N{45PDZ{IN88US=> NVXS[2k{W0GQR1XS
TE-12 NX7QR4xxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XRR2lEPTB;OUSuN|A2PSEQvF2= MV;TRW5ITVJ?
MDA-MB-361 NEPWUoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF[3emRKSzVyPUm2MlA2OTZizszN M2S3OXNCVkeHUh?=

... Click to View More Cell Line Experimental Data

In vivo試験 The induction of angiogenesis by bFGF is significantly inhibited by oral treatment of Lenalidomide in a dose-dependent manner. Lenalidomide significantly decreases the percentage of vascularized area from 5.16% (control group) to 2.58% (50 mg/kg). Lenalidomide significantly reduces the calculated total MVL from 21.07 (control) to 8.11 (50 mg/kg). Lenalidomide significantly inhibites HUVEC migration through the fibronectin-coated membranes towards 0.1 ng/mL of bFGF at 100 μM, 1 ng/mL of VEGF at concentrations of 10 μM and 100 μM. [5]
臨床試験 Lenalidomide has entered in a Phase II clinical trial in the treatment of chronic lymphocytic leukemia.
特集

プロトコル (参考用のみ)

キナーゼアッセイ:

[1]

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))].

動物実験:

[5]

動物モデル Adult male Sprague-Dawley rats bearing HUVECs cells
製剤 0.5% DMSO
投薬量 50 mg/kg and 250 mg/kg
投与方法 Administered via i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Lenalidomide (CC-5013) SDF
分子量 259.26
化学式

C13H13N3O3

CAS No. 191732-72-6
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 52 mg/mL (200.57 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 5 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 3-(4-amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione

カスタマーフィードバック (4)


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Source , , Clin Cancer Res, 2011, 17(10): 3259–71. Lenalidomide (CC-5013) purchased from Selleck
Method Western Blot
Cell Lines MM.1S cells
Concentrations 2 µM
Incubation Time 72 h
Results MM.1S cells were incubated with AT9283 0.125 μM or lenalidomide (2 μM) or combination for 72 hours; cell lysates were subjected to immunoblotting using indicated antibodies. Combined AT9283 and lenalidomide increased cleavage of caspase-8 and PARP.

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Rating
Source Obesity, 2012, 20, 2174-85. Lenalidomide (CC-5013) purchased from Selleck
Method Western Blot
Cell Lines ob/ob mice
Concentrations 50 mg/kg/day
Incubation Time 3 d
Results Although lenalidomide itself did not exert any effect on the expression of these proteins, it significantly attenuated or ablated obesity-induced upregulation of TNF-α, IL-6, Fas, and cleaved caspase-3 without any effect on FasL.

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Rating
Source Harvard Medical School. Lenalidomide (CC-5013) purchased from Selleck
Method AnnexinV/PI staining, Western blotting
Cell Lines MM.1S cells
Concentrations 2 μM
Incubation Time 0-72 h
Results The analysis showed an increase (55.7%) of cells in early and late apoptosis after 72 hours of exposure to combined therapy. Combined AT9283 and lenalidomide increased cleavage of caspase-8 and PARP. Using western blot analysis to delineate the molecular mechanism underlying this combination, we found that combination treatment resulted in downregulation of pSTAT3 and pERK following 4 hours of treatment.

Click to enlarge
Rating
Source Harvard Medical School. Lenalidomide (CC-5013) purchased from Selleck
Method Western blotting, Cell proliferation assay
Cell Lines MM.1S cells
Concentrations 2 μM
Incubation Time 4/48 h
Results Combined therapy inhibited 3H-TdR uptake of MM.1S cells cultured in the presence of BMSCs. Interestingly, consistent with this data, We observed that AT9283 plus lenalidomide downregulated the expression of the p-STAT3 and p-ERK in MM.1S cells cultured with BMSCs.

文献中の引用 (22)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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