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 MknlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYC1[mhuUUN3ME2yMlE2ODN6IN88US=> MmrIV2FPT0WU
L-363 NFPhNZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnqUmFwUUN3ME2yMlkzOjF{IN88US=> M1LDVnNCVkeHUh?=
JAR MkfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTMblY3UUN3ME2yMlk4ODBzIN88US=> Mk\RV2FPT0WU
EoL-1-cell M3XZfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPNTWM2OD12LkGwOVE2KM7:TR?= MULTRW5ITVJ?
BT-549 NYfVR5Z3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTZwMkG4OFkh|ryP M3\lSHNCVkeHUh?=
SK-NEP-1 NF;LXZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnm2TWM2OD15Lki5OVEzKM7:TR?= MV3TRW5ITVJ?
BV-173 NXHafFVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\FZWlEPTB;OD62O|U5PSEQvF2= M3mxd3NCVkeHUh?=
HMV-II MlzNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vHd2lEPTB;MUCuNFE4OiEQvF2= M4rXXHNCVkeHUh?=
HCC1806 M{DPd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonFTWM2OD1zMT60OFY4KM7:TR?= MnO2V2FPT0WU
KASUMI-1 Mn;2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkKxTWM2OD1zMT61O|Eh|ryP MW\TRW5ITVJ?
SK-MEL-28 M3vXZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnlfW8{UUN3ME2xNU46PzZ2IN88US=> M2\FRnNCVkeHUh?=
RPMI-8226 M1fJbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTF{Lk[yOFEh|ryP NYnPWJJEW0GQR1XS
T47D NWH1coVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Xre2lEPTB;MUOuNlA6QSEQvF2= NYXaNIFHW0GQR1XS
HOP-62 MlPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTF|LkS4JO69VQ>? M17Zd3NCVkeHUh?=
A2058 NI[1dVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnTdlhUUUN3ME2xN{45OTl7IN88US=> MU\TRW5ITVJ?
SW620 NFnxdHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULGdlZqUUN3ME2xOE4zPDd|IN88US=> NELJU3ZUSU6JRWK=
LCLC-103H MkDTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTJZo9PUUN3ME2xOE41QDl{IN88US=> MUHTRW5ITVJ?
HAL-01 NGrrboRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVr6[o5QUUN3ME2xOE42Pzl4IN88US=> NETG[41USU6JRWK=
PANC-08-13 M{SwcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn[4TWM2OD1zND65NVA5KM7:TR?= Mn3rV2FPT0WU
COLO-684 M1PKfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPW[FNpUUN3ME2xOU4{QTd7IN88US=> NEDXOGpUSU6JRWK=
DEL MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnpTWM2OD1zNT60PVkh|ryP NVHqSIJzW0GQR1XS
K5 NFL1VW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF:2SYlKSzVyPUG2MlE1QDZizszN NFTqcFRUSU6JRWK=
SK-MEL-24 M{\yNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUew[G5mUUN3ME2xOk41PjV{IN88US=> NVn1d4dlW0GQR1XS
ACN Mn\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvsTWM2OD1zNj61Nlk4KM7:TR?= Ml3nV2FPT0WU
H9 M1TT[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\ETWM2OD1zNj62NlYh|ryP MoHlV2FPT0WU
EM-2 M17ybGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTF5LkG0N{DPxE1? NX\oeodLW0GQR1XS
HSC-4 NUjkWoZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrtTWM2OD1zNz62OlAyKM7:TR?= M3HPSXNCVkeHUh?=
IGROV-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnqyTWM2OD1zNz63PFMh|ryP NU\w[|diW0GQR1XS
TE-1 NH71TGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTF5Lkm5Olgh|ryP MmPoV2FPT0WU
LN-405 MnHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1joc2lEPTB;MUmuPVA4PiEQvF2= MUXTRW5ITVJ?
MSTO-211H MoixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTJyLkO1O|Mh|ryP NF;DT|lUSU6JRWK=
MOLT-4 NUfheIVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTPTWM2OD1{MD61O|U6KM7:TR?= M4DzT3NCVkeHUh?=
RS4-11 NUL2WXV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfDb|gzUUN3ME2yNk4yPTZ|IN88US=> Mn3WV2FPT0WU
ES3 NEjaPZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rTPGlEPTB;MkKuOlk3OyEQvF2= MWfTRW5ITVJ?
SBC-1 MoTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTJ|Lki2PVYh|ryP M4DHUnNCVkeHUh?=
CTV-1 NYDJcXV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUj5XFFJUUN3ME2yOU4xOTR7IN88US=> M4jNUHNCVkeHUh?=
HuP-T3 NFi2ZoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH32UZlKSzVyPUK1MlQxODlizszN MlHJV2FPT0WU
HCC2218 NVLZdVVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvVd2Q3UUN3ME2yOU42PDB5IN88US=> MlzDV2FPT0WU
HDLM-2 MlHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnybmJKSzVyPUK4MlIxOjZizszN MlLsV2FPT0WU
ABC-1 M{nySGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXYSJliUUN3ME2yPU43QTd2IN88US=> NHX1OGlUSU6JRWK=
MV-4-11 NEnT[ZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTYcFZKSzVyPUK5Mlc{OTdizszN NX24eIJQW0GQR1XS
WM-115 MliwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;wUWlEPTB;M{CuN|A6QSEQvF2= MWrTRW5ITVJ?
SW1990 M1\WXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYW5UZdYUUN3ME2zNE4{OyEQvF2= MWXTRW5ITVJ?
HCC70 NF;xWFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vxVmlEPTB;M{CuO|M1PiEQvF2= NXXHNlRNW0GQR1XS
KYSE-520 MonGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPSTWM2OD1|MD64PFM6KM7:TR?= Mk\xV2FPT0WU
JEG-3 Mn3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTNzLkG2NVQh|ryP NITsSpZUSU6JRWK=
C8166 NYLPUINtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnW0TWM2OD1|MT6yNlc1KM7:TR?= MYfTRW5ITVJ?
SK-OV-3 M{Hjc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NED1cIlKSzVyPUOxMlY4PTVizszN MVfTRW5ITVJ?
NCI-H526 MkDIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLJZoZKSzVyPUOyMlY5OyEQvF2= NH;YRolUSU6JRWK=
NKM-1 MnvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXmSFVKSzVyPUOyMlk2PjhizszN MXvTRW5ITVJ?
ECC10 MlPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfhfYw2UUN3ME2zOE44PDR|IN88US=> MkLVV2FPT0WU
A2780 NFfCUFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLqeFVKSzVyPUO1MlM3ODFizszN NUjOU3ZCW0GQR1XS
KY821 NXTwVXJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPLO2dKSzVyPUO1Mlc3QDFizszN M3K5c3NCVkeHUh?=
MKN1 NIW3c2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLQNpNbUUN3ME2zOk4zOTN5IN88US=> NU\hXGd5W0GQR1XS
EKVX NHjhXIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;IUHdSUUN3ME2zO{41OjF{IN88US=> M4HBUHNCVkeHUh?=
EW-16 M4HqXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2i2Z2lEPTB;M{iuN|g5PSEQvF2= M3Tn[nNCVkeHUh?=
CTB-1 MofpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmr1TWM2OD1|OT63O|g6KM7:TR?= MVfTRW5ITVJ?
COR-L105 M2LqcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPafm9NUUN3ME20NE41PzR4IN88US=> MlTOV2FPT0WU
NCI-SNU-5 NVrOb3I3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3qOHB2UUN3ME20NU4zODZ7IN88US=> NYLtR|JYW0GQR1XS
Mewo M{ftN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;1VGlEPTB;NEGuPVg4OSEQvF2= NYfIOYs2W0GQR1XS
BCPAP M1ywcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTR|Lke5NVch|ryP NXnQ[WRGW0GQR1XS
KARPAS-45 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37kfGlEPTB;NESuNlc4PiEQvF2= NHTWco5USU6JRWK=
NCI-H1693 M{nnO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIr3VGxKSzVyPUS2MlY6QDZizszN MmL3V2FPT0WU
H-EMC-SS NFHndXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vkSWlEPTB;NEiuN|IzPCEQvF2= MW\TRW5ITVJ?
697 MkXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnwUVZKSzVyPUWwMlM2PDVizszN MUTTRW5ITVJ?
KP-N-YS NV\3UGo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HKSGlEPTB;NUKuN|E1OiEQvF2= NYO1[mh3W0GQR1XS
NCI-H1304 NYP0T4RsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTV{LkewNlQh|ryP NH3WWYxUSU6JRWK=
NOS-1 NUHLPJNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPJVINzUUN3ME21Nk45PTV7IN88US=> NFfh[|RUSU6JRWK=
NCI-H2342 MoHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{Did2lEPTB;NUOuNFUxQCEQvF2= NG\TdYNUSU6JRWK=
KYSE-270 M3zpbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTV|Lk[zOlQh|ryP M1;5fHNCVkeHUh?=
LU-135 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnj3TWM2OD13NT6xPFU{KM7:TR?= M160UXNCVkeHUh?=
OE33 NFvwW|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjBOZhKSzVyPUW1MlgyQCEQvF2= M3LvVHNCVkeHUh?=
ML-2 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEf0WlJKSzVyPUW1Mlk1QDlizszN M{jkXXNCVkeHUh?=
KMOE-2 Moi5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDwPVRKSzVyPUW2MlI5QTNizszN NWPpSXV5W0GQR1XS
Daoy M{jY[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nITWlEPTB;NU[uN|IxPCEQvF2= NVH5Olg4W0GQR1XS
KNS-62 NV:xdFJsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDVb3kyUUN3ME21O{4xOTR{IN88US=> MnniV2FPT0WU
NBsusSR NVzDVI9LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPDTWM2OD13Nz61O|A2KM7:TR?= NVj0OlJ7W0GQR1XS
UACC-257 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTV6Lk[yOlQh|ryP NFHaR5VUSU6JRWK=
LU-139 NW\qRnp7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[1TWM2OD13OD64NlYh|ryP NVPHRWFoW0GQR1XS
CAL-85-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjGOJltUUN3ME21PE45PjR|IN88US=> NHf5SHhUSU6JRWK=
NCI-H720 MoXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWj3ZnQ1UUN3ME21PE45QTR{IN88US=> M4TI[HNCVkeHUh?=
MLMA MoKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;RNlhKSzVyPUW5MlA6OSEQvF2= NVnZeWp4W0GQR1XS
A3-KAW NF\PcXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnz3TWM2OD13OT6yPFA6KM7:TR?= NXGwVmtnW0GQR1XS
Ramos-2G6-4C10 MoXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPCPHRbUUN3ME21PU43Ojh5IN88US=> M4GybHNCVkeHUh?=
A388 M13jNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorNTWM2OD14MD60OFkh|ryP MV7TRW5ITVJ?
LAMA-84 MmrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33SRWlEPTB;NkCuPVkxPSEQvF2= MULTRW5ITVJ?
GCT MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moi2TWM2OD14MT6wO|g3KM7:TR?= M{nVUHNCVkeHUh?=
K-562 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPlXZpKSzVyPU[xMlU{OzNizszN NFfCdIRUSU6JRWK=
NCI-H1666 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlL0TWM2OD14MT64O|Uh|ryP MkfMV2FPT0WU
NCI-H1993 Mn7aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjNU5JKSzVyPU[zMlQxPDNizszN NVv3N4FoW0GQR1XS
NCI-H358 NF\NNIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmSyTWM2OD14NT6wNVIyKM7:TR?= MnHYV2FPT0WU
NB6 NVLKcnYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzrVZNKSzVyPU[1Mlk5QCEQvF2= MnvRV2FPT0WU
HCE-T NXu2UnEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTZ5LkC3PVgh|ryP MVHTRW5ITVJ?
DOK MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnFZ2JNUUN3ME22O{41QTR6IN88US=> NWHRTJIyW0GQR1XS
HT-1376 M3fVWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3u5NmlEPTB;NkmuPFMyPCEQvF2= NXewcXQyW0GQR1XS
NEC8 NG[0dlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnGeFVKSzVyPUewMlEzPDNizszN M1W0ZXNCVkeHUh?=
G-402 M2TSSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXwPXdLUUN3ME23NE46Ozl3IN88US=> M{HrO3NCVkeHUh?=
GR-ST M4PicWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITmeZhKSzVyPUexMlE4OiEQvF2= MVfTRW5ITVJ?
QIMR-WIL NX\HZYlUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnDNplRUUN3ME23NU41PDN2IN88US=> M{HEZXNCVkeHUh?=
CHP-212 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIe2eFRKSzVyPUexMlk3PSEQvF2= MVTTRW5ITVJ?
KU812 NGS5eWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXwTWM2OD15Mj65O|AzKM7:TR?= M4HWWnNCVkeHUh?=
Becker NGr0e2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\QdI5NUUN3ME23N{4yPDh7IN88US=> MV;TRW5ITVJ?
ChaGo-K-1 MnvwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIX3TYdKSzVyPUe0Mlc1QDZizszN MWrTRW5ITVJ?
A498 NH\TZVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\jUYpnUUN3ME23OE46OzB6IN88US=> MkTjV2FPT0WU
NCI-H69 NUTEdHd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2P1WGlEPTB;N{WuO|Y3OyEQvF2= MkfzV2FPT0WU
NCI-H209 NWq3cIZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHkeFZKSzVyPUe4MlYyPDdizszN NH;2N4lUSU6JRWK=
CAL-33 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{C3V2lEPTB;N{iuPVk{QSEQvF2= MYXTRW5ITVJ?
COLO-680N MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPiOFNKSzVyPUe5MlExODdizszN M1Hm[XNCVkeHUh?=
D-283MED M{nCRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7nTWM2OD15OT64NVIh|ryP Mn30V2FPT0WU
ATN-1 MoHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHhbGduUUN3ME24NU4yOTh5IN88US=> NIXMNHVUSU6JRWK=
NCI-N87 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRThzLkeyPVYh|ryP NXjoT4szW0GQR1XS
MHH-NB-11 NGnWd2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XC[GlEPTB;OEGuPFg1QSEQvF2= NVzKSm5zW0GQR1XS
HEL NHHDSoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTh{LkSxN|Qh|ryP NYryfHlrW0GQR1XS
NB69 MoXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\KeoJKSzVyPUizMlAxOzNizszN M2nlWXNCVkeHUh?=
MPP-89 NYHWVVNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTh|LkK1O|Uh|ryP MlzwV2FPT0WU
COLO-829 MnvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXz3bIxwUUN3ME24OU41QTF{IN88US=> NVTx[mFtW0GQR1XS
ONS-76 MnqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TNdmlEPTB;OEWuO|kxQCEQvF2= MnXiV2FPT0WU
EW-3 M4\VSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\UZmlEPTB;OE[uNlA{OiEQvF2= MWjTRW5ITVJ?
EW-11 M4rmb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTh4LkSzN|Yh|ryP NHW1eWlUSU6JRWK=
SW900 M2HLXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfyb|ZKSzVyPUi3MlIxPTNizszN MlrkV2FPT0WU
MOLT-13 NXn2RpFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTjdXNKSzVyPUi3MlIzPDNizszN NUnSPGxHW0GQR1XS
HuP-T4 NVGwcoF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHGwVG9KSzVyPUmxMlA1ODVizszN MXLTRW5ITVJ?
HCC1419 NHvBNW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDzNW9KSzVyPUmxMlY{PzRizszN M4XOdnNCVkeHUh?=
CAL-72 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDJ[VQyUUN3ME25Nk4xOjF7IN88US=> NFexXllUSU6JRWK=
Mo-T NXXIOVNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjnXWV4UUN3ME25Nk44Pjl5IN88US=> M{\zN3NCVkeHUh?=
OC-314 MkPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{ntTGlEPTB;OUKuPFgzOSEQvF2= NFH2UHRUSU6JRWK=
BHT-101 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPhXmdKSzVyPUmzMlEh|ryP NFXIcIlUSU6JRWK=
EW-18 Mm[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFSzUYZKSzVyPUmzMlg1PjJizszN NXLOcWg3W0GQR1XS
TE-12 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17nVGlEPTB;OUSuN|A2PSEQvF2= MlTyV2FPT0WU
MDA-MB-361 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfzTWM2OD17Nj6wOVE3KM7:TR?= M4e1dXNCVkeHUh?=

... 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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Rating
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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