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 MnXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPiXmpEUUN3ME2yMlE2ODN6IN88US=> MVzTRW5ITVJ?
L-363 Mkm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTJwOUKyNVIh|ryP MmjiV2FPT0WU
JAR MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPTcJJSUUN3ME2yMlk4ODBzIN88US=> MVTTRW5ITVJ?
EoL-1-cell MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIntZZBKSzVyPUSuNVA2OTVizszN M3PVOHNCVkeHUh?=
BT-549 NF7x[XBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rLfGlEPTB;Nj6yNVg1QSEQvF2= NYfQN2xJW0GQR1XS
SK-NEP-1 M1jvUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTdwOEm1NVIh|ryP MYjTRW5ITVJ?
BV-173 MnzaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vHdmlEPTB;OD62O|U5PSEQvF2= NHS0V2NUSU6JRWK=
HMV-II Mk\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEP1e4JKSzVyPUGwMlAyPzJizszN NXTNXGh[W0GQR1XS
HCC1806 NWfDd3E5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\MbGlEPTB;MUGuOFQ3PyEQvF2= MoLqV2FPT0WU
KASUMI-1 NGjneFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnvTXlKSzVyPUGxMlU4OSEQvF2= MknlV2FPT0WU
SK-MEL-28 NH3xVodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTFzLkm3OlQh|ryP M{HUWXNCVkeHUh?=
RPMI-8226 NGW0[5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3G0[GlEPTB;MUKuOlI1OSEQvF2= NVHaNoRbW0GQR1XS
T47D M4DY[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTF|LkKwPVkh|ryP MV3TRW5ITVJ?
HOP-62 M3P3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\LOGlEPTB;MUOuOFgh|ryP NFHDb49USU6JRWK=
A2058 M4r6c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DNUGlEPTB;MUOuPFE6QSEQvF2= MlL4V2FPT0WU
SW620 M4PEd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{C4NWlEPTB;MUSuNlQ4OyEQvF2= MnuzV2FPT0WU
LCLC-103H M{\H[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\NOlVKSzVyPUG0MlQ5QTJizszN M1vpO3NCVkeHUh?=
HAL-01 NFnvNHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HjRmlEPTB;MUSuOVc6PiEQvF2= NVrSOmdiW0GQR1XS
PANC-08-13 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\pWolKSzVyPUG0MlkyODhizszN NEjoSmpUSU6JRWK=
COLO-684 M1r6eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3y0dWlEPTB;MUWuN|k4QSEQvF2= M1H1cXNCVkeHUh?=
DEL MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LMNGlEPTB;MUWuOFk6KM7:TR?= NEPtb21USU6JRWK=
K5 NXW1OVRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\3OGlEPTB;MU[uNVQ5PiEQvF2= M2P0dnNCVkeHUh?=
SK-MEL-24 NFnDUXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTF4LkS2OVIh|ryP M4PGPXNCVkeHUh?=
ACN NHXoclZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjTTWM2OD1zNj61Nlk4KM7:TR?= NFS0W4pUSU6JRWK=
H9 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzOW|dKSzVyPUG2MlYzPiEQvF2= NWjKS4JKW0GQR1XS
EM-2 M13MfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DZVmlEPTB;MUeuNVQ{KM7:TR?= M17tS3NCVkeHUh?=
HSC-4 M1fUVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXQUW1jUUN3ME2xO{43PjBzIN88US=> NF7O[2lUSU6JRWK=
IGROV-1 NUCzUmFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTF5Lke4N{DPxE1? NXTOW25vW0GQR1XS
TE-1 M3PrRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHv1W|JKSzVyPUG3Mlk6PjhizszN Moe3V2FPT0WU
LN-405 M3m2cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPqTWM2OD1zOT65NFc3KM7:TR?= MkLoV2FPT0WU
MSTO-211H MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nsWWlEPTB;MkCuN|U4OyEQvF2= NVH1S|lHW0GQR1XS
MOLT-4 NIL0UIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPzTWM2OD1{MD61O|U6KM7:TR?= NYDWSVhtW0GQR1XS
RS4-11 NUK3VVB2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rsfWlEPTB;MkKuNVU3OyEQvF2= NWTxO|dtW0GQR1XS
ES3 M4W5WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4eyRWlEPTB;MkKuOlk3OyEQvF2= M3vodnNCVkeHUh?=
SBC-1 NFjsd3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Tae2lEPTB;MkOuPFY6PiEQvF2= NXTHU2lDW0GQR1XS
CTV-1 M3ft[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTJ3LkCxOFkh|ryP MoLTV2FPT0WU
HuP-T3 MkTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4f0OWlEPTB;MkWuOFAxQSEQvF2= M3zVcHNCVkeHUh?=
HCC2218 M1XONGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\LUHQ1UUN3ME2yOU42PDB5IN88US=> NHz0bJNUSU6JRWK=
HDLM-2 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLXNplKSzVyPUK4MlIxOjZizszN MlLyV2FPT0WU
ABC-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3L1NWlEPTB;MkmuOlk4PCEQvF2= NEHkd4pUSU6JRWK=
MV-4-11 NILqfHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonVTWM2OD1{OT63N|E4KM7:TR?= NVfROnlSW0GQR1XS
WM-115 M1jqdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkj5TWM2OD1|MD6zNFk6KM7:TR?= MXjTRW5ITVJ?
SW1990 NWHR[GNRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HYb2lEPTB;M{CuN|Mh|ryP M3mwcnNCVkeHUh?=
HCC70 MnK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HVc2lEPTB;M{CuO|M1PiEQvF2= NX32XnRlW0GQR1XS
KYSE-520 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFW5[FdKSzVyPUOwMlg5OzlizszN M{HO[HNCVkeHUh?=
JEG-3 M3vCU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zXd2lEPTB;M{GuNVYyPCEQvF2= MkfrV2FPT0WU
C8166 MnTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPLXZNzUUN3ME2zNU4zOjd2IN88US=> Mlf3V2FPT0WU
SK-OV-3 MkTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jsdGlEPTB;M{GuOlc2PSEQvF2= MkfmV2FPT0WU
NCI-H526 NV;OfHdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn[2TWM2OD1|Mj62PFMh|ryP MlT5V2FPT0WU
NKM-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfmWFhKSzVyPUOyMlk2PjhizszN M{jwT3NCVkeHUh?=
ECC10 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;UPVhTUUN3ME2zOE44PDR|IN88US=> M1K3SXNCVkeHUh?=
A2780 M{LLT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPPXYpKSzVyPUO1MlM3ODFizszN M{fL[3NCVkeHUh?=
KY821 NHPEe5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rNdWlEPTB;M{WuO|Y5OSEQvF2= NVHKRYtGW0GQR1XS
MKN1 M3joPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moj4TWM2OD1|Nj6yNVM4KM7:TR?= MULTRW5ITVJ?
EKVX NFXURnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1ywUWlEPTB;M{euOFIyOiEQvF2= Ml\oV2FPT0WU
EW-16 MkX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDvT5RmUUN3ME2zPE4{QDh3IN88US=> NVfxT4lOW0GQR1XS
CTB-1 Mn7GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXGzeXFGUUN3ME2zPU44Pzh7IN88US=> NX\uTHBtW0GQR1XS
COR-L105 NI\WcY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnH6TWM2OD12MD60O|Q3KM7:TR?= MXTTRW5ITVJ?
NCI-SNU-5 NW[5flFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;hNZhKSzVyPUSxMlIxPjlizszN NYfITVJ7W0GQR1XS
Mewo NH\obZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjGW3lSUUN3ME20NU46QDdzIN88US=> MkHRV2FPT0WU
BCPAP MkOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTR|Lke5NVch|ryP NEezW2ZUSU6JRWK=
KARPAS-45 NFjKflFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HPeWlEPTB;NESuNlc4PiEQvF2= MWfTRW5ITVJ?
NCI-H1693 NVTBfnQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\DZmlEPTB;NE[uOlk5PiEQvF2= NEHEfoxUSU6JRWK=
H-EMC-SS NELTVpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLIbG9KSzVyPUS4MlMzOjRizszN MYLTRW5ITVJ?
697 NYL3WlFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTMTWM2OD13MD6zOVQ2KM7:TR?= MWjTRW5ITVJ?
KP-N-YS MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnaTZVjUUN3ME21Nk4{OTR{IN88US=> NYq0dm9uW0GQR1XS
NCI-H1304 NWj6VVNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjJTWM2OD13Mj63NFI1KM7:TR?= NETDcW9USU6JRWK=
NOS-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoSzTWM2OD13Mj64OVU6KM7:TR?= M1PqOnNCVkeHUh?=
NCI-H2342 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlezTWM2OD13Mz6wOVA5KM7:TR?= MX;TRW5ITVJ?
KYSE-270 NYLGZ2hLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Hy[GlEPTB;NUOuOlM3PCEQvF2= Mn[yV2FPT0WU
LU-135 NES5SZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULwZodPUUN3ME21OU4yQDV|IN88US=> NHeweY5USU6JRWK=
OE33 NFfaWmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3KwTGlEPTB;NUWuPFE5KM7:TR?= NHv5WI9USU6JRWK=
ML-2 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TwbWlEPTB;NUWuPVQ5QSEQvF2= NXnCZ4RHW0GQR1XS
KMOE-2 NHe1U|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUixV5Q3UUN3ME21Ok4zQDl|IN88US=> NETEUoNUSU6JRWK=
Daoy M2DpeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTV4LkOyNFQh|ryP MnT6V2FPT0WU
KNS-62 MoXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknzTWM2OD13Nz6wNVQzKM7:TR?= NVjCfHZqW0GQR1XS
NBsusSR MnKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rM[GlEPTB;NUeuOVcxPSEQvF2= MVrTRW5ITVJ?
UACC-257 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTV6Lk[yOlQh|ryP NXvufoUzW0GQR1XS
LU-139 Ml3FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFf3WFFKSzVyPUW4MlgzPiEQvF2= MmHHV2FPT0WU
CAL-85-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrMTWM2OD13OD64OlQ{KM7:TR?= Ml3EV2FPT0WU
NCI-H720 NHvxeoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLoR|RKSzVyPUW4Mlg6PDJizszN NGLMOpJUSU6JRWK=
MLMA MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{eyfWlEPTB;NUmuNFkyKM7:TR?= NUf6UmtLW0GQR1XS
A3-KAW NEX2Z25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jwZ2lEPTB;NUmuNlgxQSEQvF2= NITqbWdUSU6JRWK=
Ramos-2G6-4C10 MnvES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXJTWM2OD13OT62Nlg4KM7:TR?= NXTt[GZXW0GQR1XS
A388 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn6xTWM2OD14MD60OFkh|ryP NInhUWZUSU6JRWK=
LAMA-84 NH3XXI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvDVoplUUN3ME22NE46QTB3IN88US=> Mn;yV2FPT0WU
GCT MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLrbmpKSzVyPU[xMlA4QDZizszN NWjQSIlbW0GQR1XS
K-562 MnPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH6zc29KSzVyPU[xMlU{OzNizszN MWjTRW5ITVJ?
NCI-H1666 NXnjXZI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTZzLki3OUDPxE1? NVnyRYV6W0GQR1XS
NCI-H1993 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn[0TWM2OD14Mz60NFQ{KM7:TR?= MXnTRW5ITVJ?
NCI-H358 MoDwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\OTGZKSzVyPU[1MlAyOjFizszN MkL2V2FPT0WU
NB6 M1OzXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2j1U2lEPTB;NkWuPVg5KM7:TR?= M4mzVnNCVkeHUh?=
HCE-T MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PvdmlEPTB;NkeuNFc6QCEQvF2= NI\jbmRUSU6JRWK=
DOK NGX4SI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTZ5LkS5OFgh|ryP NX7vcHcxW0GQR1XS
HT-1376 NF;Qdm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofMTWM2OD14OT64N|E1KM7:TR?= MYLTRW5ITVJ?
NEC8 NXrkPHpET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LCN2lEPTB;N{CuNVI1OyEQvF2= M3;FS3NCVkeHUh?=
G-402 NETaTHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\lR|I3UUN3ME23NE46Ozl3IN88US=> NFXGOoxUSU6JRWK=
GR-ST NH7HVWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzKeFByUUN3ME23NU4yPzJizszN MYnTRW5ITVJ?
QIMR-WIL MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXJTWM2OD15MT60OFM1KM7:TR?= Mom5V2FPT0WU
CHP-212 NYjRR5FET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTdzLkm2OUDPxE1? MnrmV2FPT0WU
KU812 M4rVRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfPXmxzUUN3ME23Nk46PzB{IN88US=> MWHTRW5ITVJ?
Becker MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTlNJVKSzVyPUezMlE1QDlizszN MofWV2FPT0WU
ChaGo-K-1 NICxXGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fz[GlEPTB;N{SuO|Q5PiEQvF2= Mn7wV2FPT0WU
A498 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHtTWM2OD15ND65N|A5KM7:TR?= MnnyV2FPT0WU
NCI-H69 NUDvRlh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTd3Lke2OlMh|ryP NVXSVlZlW0GQR1XS
NCI-H209 M2HJXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTd6Lk[xOFch|ryP MYDTRW5ITVJ?
CAL-33 NEHWTG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NECyNW1KSzVyPUe4Mlk6OzlizszN M2m2c3NCVkeHUh?=
COLO-680N NIe3NodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jhSmlEPTB;N{muNVAxPyEQvF2= M4TsUnNCVkeHUh?=
D-283MED Mo\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvGOZVFUUN3ME23PU45OTJizszN M336VnNCVkeHUh?=
ATN-1 Ml3uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXucZNGUUN3ME24NU4yOTh5IN88US=> NFfsW5ZUSU6JRWK=
NCI-N87 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\TTXRKSzVyPUixMlczQTZizszN MoPDV2FPT0WU
MHH-NB-11 NWjLeY5TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\NZplKSzVyPUixMlg5PDlizszN NIi1RnFUSU6JRWK=
HEL M3:wfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX:0RmxxUUN3ME24Nk41OTN2IN88US=> M1S0VnNCVkeHUh?=
NB69 M3TtfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HMOmlEPTB;OEOuNFA{OyEQvF2= NIn4d2VUSU6JRWK=
MPP-89 NGfNXZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fvTWlEPTB;OEOuNlU4PSEQvF2= Mn3yV2FPT0WU
COLO-829 NFe4fItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfnbWtvUUN3ME24OU41QTF{IN88US=> M1WzcXNCVkeHUh?=
ONS-76 NVq3T5VpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPvRVBLUUN3ME24OU44QTB6IN88US=> MXPTRW5ITVJ?
EW-3 M1\qb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LuPWlEPTB;OE[uNlA{OiEQvF2= MYnTRW5ITVJ?
EW-11 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHNTWM2OD16Nj60N|M3KM7:TR?= NEfONXRUSU6JRWK=
SW900 NInERY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjlUVVKSzVyPUi3MlIxPTNizszN NUfMcINIW0GQR1XS
MOLT-13 M4HBSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\OTWM2OD16Nz6yNlQ{KM7:TR?= NUfFeXpGW0GQR1XS
HuP-T4 M4HMN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvCb|NYUUN3ME25NU4xPDB3IN88US=> M{ezRXNCVkeHUh?=
HCC1419 NWOwT4FvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkS5TWM2OD17MT62N|c1KM7:TR?= Mmq1V2FPT0WU
CAL-72 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLEeopMUUN3ME25Nk4xOjF7IN88US=> MlPDV2FPT0WU
Mo-T MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7sTWM2OD17Mj63Olk4KM7:TR?= NUnxPWJIW0GQR1XS
OC-314 NFjmXVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTl{Lki4NlEh|ryP Mmn6V2FPT0WU
BHT-101 MlHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTl|LkGg{txO M13PNHNCVkeHUh?=
EW-18 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfhTWM2OD17Mz64OFYzKM7:TR?= M2fv[XNCVkeHUh?=
TE-12 Ml;mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonGTWM2OD17ND6zNFU2KM7:TR?= NVvoUWk{W0GQR1XS
MDA-MB-361 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDGTWM2OD17Nj6wOVE3KM7:TR?= MoXvV2FPT0WU

... 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)

Frequently Asked Questions

  • Question 1
    What is the formulation for mouse injection(i.p.)?

    Answer: 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.

  • Question 2
    what is the procedure to resuspend this compound?

    Answer: 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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