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 M4nMOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPLTWM2OD1{LkG1NFM5KM7:TR?= MUPTRW5ITVJ?
L-363 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3r6fWlEPTB;Mj65NlIyOiEQvF2= NX3oRWxpW0GQR1XS
JAR MmDTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXwZmhIUUN3ME2yMlk4ODBzIN88US=> MmXJV2FPT0WU
EoL-1-cell M2XBS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoexTWM2OD12LkGwOVE2KM7:TR?= NH;Tb4JUSU6JRWK=
BT-549 NVT5OJRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TpdWlEPTB;Nj6yNVg1QSEQvF2= M4PVc3NCVkeHUh?=
SK-NEP-1 M1jEN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfnVG1KSzVyPUeuPFk2OTJizszN M{DHRXNCVkeHUh?=
BV-173 NIDSb21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PMUmlEPTB;OD62O|U5PSEQvF2= NF;VTGRUSU6JRWK=
HMV-II NFqz[2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTFyLkCxO|Ih|ryP M3nYUXNCVkeHUh?=
HCC1806 NITrclZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NID4elJKSzVyPUGxMlQ1PjdizszN M2\5bXNCVkeHUh?=
KASUMI-1 NUP3[pN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DzVmlEPTB;MUGuOVcyKM7:TR?= MlnyV2FPT0WU
SK-MEL-28 NGrPPHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPWbodKSzVyPUGxMlk4PjRizszN M2G3XnNCVkeHUh?=
RPMI-8226 NVTFe5FET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljnTWM2OD1zMj62NlQyKM7:TR?= NILxZnpUSU6JRWK=
T47D M1LsZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTF|LkKwPVkh|ryP NFvPe4VUSU6JRWK=
HOP-62 M4K5cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTF|LkS4JO69VQ>? M4jTRXNCVkeHUh?=
A2058 NV33WFVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTF|LkixPVkh|ryP NYXBPGFVW0GQR1XS
SW620 Mm\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXSS4s{UUN3ME2xOE4zPDd|IN88US=> MX\TRW5ITVJ?
LCLC-103H MmqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVX2cXI3UUN3ME2xOE41QDl{IN88US=> MXXTRW5ITVJ?
HAL-01 NWi0SGljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfON5hKSzVyPUG0MlU4QTZizszN NXHvZ4VJW0GQR1XS
PANC-08-13 NHziOmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTF2LkmxNFgh|ryP NIf0WnRUSU6JRWK=
COLO-684 NGfKT41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rye2lEPTB;MUWuN|k4QSEQvF2= NG\ydIxUSU6JRWK=
DEL MnO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzHSWdKSzVyPUG1MlQ6QSEQvF2= NVXaUZZqW0GQR1XS
K5 MmiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTF4LkG0PFYh|ryP NXXCSJRnW0GQR1XS
SK-MEL-24 NVThXo9wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jHUWlEPTB;MU[uOFY2OiEQvF2= MmjjV2FPT0WU
ACN NF65XHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TQTGlEPTB;MU[uOVI6PyEQvF2= Mki3V2FPT0WU
H9 NHvrRWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTF4Lk[yOkDPxE1? MoPWV2FPT0WU
EM-2 NFX1UYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTF5LkG0N{DPxE1? M4HxS3NCVkeHUh?=
HSC-4 Ml\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTNTWM2OD1zNz62OlAyKM7:TR?= M2rpXXNCVkeHUh?=
IGROV-1 NHjafldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mme5TWM2OD1zNz63PFMh|ryP NHqydFVUSU6JRWK=
TE-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fqTGlEPTB;MUeuPVk3QCEQvF2= MoTSV2FPT0WU
LN-405 M2S1NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTF7LkmwO|Yh|ryP MnLUV2FPT0WU
MSTO-211H NHjqbIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTJyLkO1O|Mh|ryP NUTi[pZoW0GQR1XS
MOLT-4 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\Ue|VKSzVyPUKwMlU4PTlizszN NGLDcIlUSU6JRWK=
RS4-11 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fTO2lEPTB;MkKuNVU3OyEQvF2= NIDxOGxUSU6JRWK=
ES3 NFj1[3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDITHpKSzVyPUKyMlY6PjNizszN M3nJSXNCVkeHUh?=
SBC-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfNdWVKSzVyPUKzMlg3QTZizszN NGfPW3hUSU6JRWK=
CTV-1 M1W1e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorHTWM2OD1{NT6wNVQ6KM7:TR?= M{fuUnNCVkeHUh?=
HuP-T3 M{TQb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{H0PGlEPTB;MkWuOFAxQSEQvF2= MWPTRW5ITVJ?
HCC2218 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVm0bmd4UUN3ME2yOU42PDB5IN88US=> M4mwN3NCVkeHUh?=
HDLM-2 M33oTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XpfGlEPTB;MkiuNlAzPiEQvF2= M17kbXNCVkeHUh?=
ABC-1 NVmzfoRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HYN2lEPTB;MkmuOlk4PCEQvF2= M2j6XnNCVkeHUh?=
MV-4-11 MlrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7CTWM2OD1{OT63N|E4KM7:TR?= MlG5V2FPT0WU
WM-115 NF73XG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mny0TWM2OD1|MD6zNFk6KM7:TR?= NUDh[4pkW0GQR1XS
SW1990 NV3wbFgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LsbWlEPTB;M{CuN|Mh|ryP NHHiN4lUSU6JRWK=
HCC70 M4rWfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2i3dWlEPTB;M{CuO|M1PiEQvF2= NGe1U2JUSU6JRWK=
KYSE-520 NIXCNWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDRNGljUUN3ME2zNE45QDN7IN88US=> M4fBT3NCVkeHUh?=
JEG-3 NFTudZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLOTWM2OD1|MT6xOlE1KM7:TR?= Mo[0V2FPT0WU
C8166 NGfhR4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml21TWM2OD1|MT6yNlc1KM7:TR?= MnzTV2FPT0WU
SK-OV-3 M1\qcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTNzLk[3OVUh|ryP Ml3HV2FPT0WU
NCI-H526 NEi0VZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonjTWM2OD1|Mj62PFMh|ryP M2PWZ3NCVkeHUh?=
NKM-1 M4DkcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvtTWM2OD1|Mj65OVY5KM7:TR?= MULTRW5ITVJ?
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A2780 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XyV2lEPTB;M{WuN|YxOSEQvF2= MUjTRW5ITVJ?
KY821 NUDyb25OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETTR|RKSzVyPUO1Mlc3QDFizszN MoXBV2FPT0WU
MKN1 MmTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHFOHdKSzVyPUO2MlIyOzdizszN NYjjdXhnW0GQR1XS
EKVX NFizbWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TrTWlEPTB;M{euOFIyOiEQvF2= M4P6XXNCVkeHUh?=
EW-16 MlPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTN6LkO4PFUh|ryP MUDTRW5ITVJ?
CTB-1 MmT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXGO3hKSzVyPUO5Mlc4QDlizszN NYjHb4NOW0GQR1XS
COR-L105 NH7ke3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDmTWM2OD12MD60O|Q3KM7:TR?= NX\rV5p3W0GQR1XS
NCI-SNU-5 MlfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTRzLkKwOlkh|ryP M2DxVXNCVkeHUh?=
Mewo M4\lbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY[1cFg6UUN3ME20NU46QDdzIN88US=> MX3TRW5ITVJ?
BCPAP M3z1fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\FdpJKSzVyPUSzMlc6OTdizszN NGfoOHNUSU6JRWK=
KARPAS-45 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPwTWM2OD12ND6yO|c3KM7:TR?= NIj3cJlUSU6JRWK=
NCI-H1693 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjaUGFKSzVyPUS2MlY6QDZizszN NGPLXXBUSU6JRWK=
H-EMC-SS NYDpXVRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXu5NoZRUUN3ME20PE4{OjJ2IN88US=> MUDTRW5ITVJ?
697 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2L5O2lEPTB;NUCuN|U1PSEQvF2= M1rMdXNCVkeHUh?=
KP-N-YS NGns[GpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF24fo1KSzVyPUWyMlMyPDJizszN NVLvSpBQW0GQR1XS
NCI-H1304 M2fFdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3ntNWlEPTB;NUKuO|AzPCEQvF2= M4XrVXNCVkeHUh?=
NOS-1 M3:xO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIC3NnhKSzVyPUWyMlg2PTlizszN MkO3V2FPT0WU
NCI-H2342 MnS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXPUXk{UUN3ME21N{4xPTB6IN88US=> NEXwTo5USU6JRWK=
KYSE-270 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTV|Lk[zOlQh|ryP MVHTRW5ITVJ?
LU-135 M{C1[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTVXXVzUUN3ME21OU4yQDV|IN88US=> NYj3dmFYW0GQR1XS
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ML-2 NUfiWG16T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTV3Lkm0PFkh|ryP M3zibXNCVkeHUh?=
KMOE-2 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXKTWM2OD13Nj6yPFk{KM7:TR?= Ml25V2FPT0WU
Daoy NYLob2VLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnaTWM2OD13Nj6zNlA1KM7:TR?= M2G0cnNCVkeHUh?=
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UACC-257 NELsRoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjaeXNKSzVyPUW4MlYzPjRizszN NXPzfW9yW0GQR1XS
LU-139 NFz1d2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTV6LkiyOkDPxE1? NWPXcVZsW0GQR1XS
CAL-85-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rYZmlEPTB;NUiuPFY1OyEQvF2= M2DMOnNCVkeHUh?=
NCI-H720 NHnOVJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzhbVJmUUN3ME21PE45QTR{IN88US=> NIjWOGFUSU6JRWK=
MLMA MnTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHwPI9KSzVyPUW5MlA6OSEQvF2= M{XtXnNCVkeHUh?=
A3-KAW MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTV7LkK4NFkh|ryP NXW4dHljW0GQR1XS
Ramos-2G6-4C10 NVLRWpFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvPcZpKSzVyPUW5MlYzQDdizszN M1n1NnNCVkeHUh?=
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LAMA-84 M{LjOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLqV2lKSzVyPU[wMlk6ODVizszN MV3TRW5ITVJ?
GCT MmrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTZzLkC3PFYh|ryP MXLTRW5ITVJ?
K-562 M1\TWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTZzLkWzN|Mh|ryP MYDTRW5ITVJ?
NCI-H1666 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnsOJpwUUN3ME22NU45PzVizszN NULDS3VnW0GQR1XS
NCI-H1993 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIi3OWpKSzVyPU[zMlQxPDNizszN NF34eG9USU6JRWK=
NCI-H358 NGC2bWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTZ3LkCxNlEh|ryP MYDTRW5ITVJ?
NB6 Ml;5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDTTWM2OD14NT65PFgh|ryP MofZV2FPT0WU
HCE-T NUDZV|FKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljnTWM2OD14Nz6wO|k5KM7:TR?= M{K1[HNCVkeHUh?=
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HT-1376 M1:zVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HMWWlEPTB;NkmuPFMyPCEQvF2= MkfoV2FPT0WU
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GR-ST MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTdzLkG3NkDPxE1? MX\TRW5ITVJ?
QIMR-WIL MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPLNnNZUUN3ME23NU41PDN2IN88US=> Mkn5V2FPT0WU
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Becker NELibWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTd|LkG0PFkh|ryP MYrTRW5ITVJ?
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A498 M{\Kd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTd2LkmzNFgh|ryP MYrTRW5ITVJ?
NCI-H69 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\JXWlEPTB;N{WuO|Y3OyEQvF2= NIfhXZVUSU6JRWK=
NCI-H209 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoWxTWM2OD15OD62NVQ4KM7:TR?= NYPPNZBrW0GQR1XS
CAL-33 M3Hifmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTd6Lkm5N|kh|ryP NVPTWpppW0GQR1XS
COLO-680N MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTd7LkGwNFch|ryP NXrzPI9jW0GQR1XS
D-283MED NFWz[ZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjlTWM2OD15OT64NVIh|ryP MYnTRW5ITVJ?
ATN-1 Mmf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HlW2lEPTB;OEGuNVE5PyEQvF2= NYTNcnI1W0GQR1XS
NCI-N87 NYLu[FBMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTmTWM2OD16MT63Nlk3KM7:TR?= NVTkVJdQW0GQR1XS
MHH-NB-11 NELJO2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRThzLki4OFkh|ryP M13iXnNCVkeHUh?=
HEL NU[5R4JbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnSd4NDUUN3ME24Nk41OTN2IN88US=> NVfXZ2s5W0GQR1XS
NB69 NXTPSIdWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjnU|NTUUN3ME24N{4xODN|IN88US=> MVrTRW5ITVJ?
MPP-89 NGXpWVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrDfHhKSzVyPUizMlI2PzVizszN NWTjdlZFW0GQR1XS
COLO-829 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLETWM2OD16NT60PVEzKM7:TR?= M3\ZWnNCVkeHUh?=
ONS-76 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\ZTWM2OD16NT63PVA5KM7:TR?= MnvhV2FPT0WU
EW-3 M2LaV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorZTWM2OD16Nj6yNFMzKM7:TR?= NYf3cpFIW0GQR1XS
EW-11 Mn32S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fxU2lEPTB;OE[uOFM{PiEQvF2= MVfTRW5ITVJ?
SW900 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojTTWM2OD16Nz6yNFU{KM7:TR?= NWfx[25oW0GQR1XS
MOLT-13 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVe0SIpmUUN3ME24O{4zOjR|IN88US=> M1PNRnNCVkeHUh?=
HuP-T4 M1;2V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEWyNI5KSzVyPUmxMlA1ODVizszN MX3TRW5ITVJ?
HCC1419 MknSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3CTWM2OD17MT62N|c1KM7:TR?= MlPSV2FPT0WU
CAL-72 NYPQXVA{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mny3TWM2OD17Mj6wNlE6KM7:TR?= MlP3V2FPT0WU
Mo-T MlrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVSzepREUUN3ME25Nk44Pjl5IN88US=> NEfPPHpUSU6JRWK=
OC-314 NFrSZlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1W4emlEPTB;OUKuPFgzOSEQvF2= NXrRWlU{W0GQR1XS
BHT-101 M1nx[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEeyeplKSzVyPUmzMlEh|ryP MVPTRW5ITVJ?
EW-18 M4q2cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LKW2lEPTB;OUOuPFQ3OiEQvF2= M3\2XnNCVkeHUh?=
TE-12 Ml3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HP[WlEPTB;OUSuN|A2PSEQvF2= M1nxUHNCVkeHUh?=
MDA-MB-361 M{DKPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1uxW2lEPTB;OU[uNFUyPiEQvF2= NGTlPJpUSU6JRWK=

... 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

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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