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

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製品説明

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    TNF-alpha製品生物活性の比較
  • 研究分野
  • Combination Therapy
    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 NU[xTnFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXFTWM2OD1{LkG1NFM5KM7:TR?= MlrmV2FPT0WU
L-363 M{\GZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPCTWM2OD1{LkmyNlEzKM7:TR?= NY\M[mZQW0GQR1XS
JAR NYTDNWZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnlWFdIUUN3ME2yMlk4ODBzIN88US=> MWfTRW5ITVJ?
EoL-1-cell NYP0e2tWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDodllKSzVyPUSuNVA2OTVizszN M4fCVHNCVkeHUh?=
BT-549 NV\yZ2FRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3WwPGlEPTB;Nj6yNVg1QSEQvF2= MUHTRW5ITVJ?
SK-NEP-1 Mk\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\aV3VjUUN3ME23Mlg6PTF{IN88US=> M{K0[HNCVkeHUh?=
BV-173 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRThwNke1PFUh|ryP NWniUGVnW0GQR1XS
HMV-II NHjYc2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PydWlEPTB;MUCuNFE4OiEQvF2= NUPDbWRzW0GQR1XS
HCC1806 Ml;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTFzLkS0Olch|ryP M3nGVXNCVkeHUh?=
KASUMI-1 MlqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\BWFVKSzVyPUGxMlU4OSEQvF2= NGjDV|dUSU6JRWK=
SK-MEL-28 MmfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DzR2lEPTB;MUGuPVc3PCEQvF2= Mkj5V2FPT0WU
RPMI-8226 NU[zRW83T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzOU3hWUUN3ME2xNk43OjRzIN88US=> MXPTRW5ITVJ?
T47D NUPDeHo2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvxR5FKSzVyPUGzMlIxQTlizszN MXvTRW5ITVJ?
HOP-62 MlrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLiUmFSUUN3ME2xN{41QCEQvF2= Mnz5V2FPT0WU
A2058 NEDUb4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTF|LkixPVkh|ryP NYrqVIMyW0GQR1XS
SW620 M3;OTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXsfHdKSzVyPUG0MlI1PzNizszN MlzuV2FPT0WU
LCLC-103H Ml7PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\DXpNKSzVyPUG0MlQ5QTJizszN NYTqXo9UW0GQR1XS
HAL-01 NHLXb4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTF2LkW3PVYh|ryP MYPTRW5ITVJ?
PANC-08-13 MmTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE[ySpdKSzVyPUG0MlkyODhizszN NVrhWJhlW0GQR1XS
COLO-684 NHTn[otIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDYfIYzUUN3ME2xOU4{QTd7IN88US=> Mkm5V2FPT0WU
DEL MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTF3LkS5PUDPxE1? Mmf5V2FPT0WU
K5 NV\j[mh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3ThS2lEPTB;MU[uNVQ5PiEQvF2= M1L6dnNCVkeHUh?=
SK-MEL-24 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkL3TWM2OD1zNj60OlUzKM7:TR?= M2jYVHNCVkeHUh?=
ACN MlO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7RfXE{UUN3ME2xOk42Ojl5IN88US=> M2DKV3NCVkeHUh?=
H9 NWjRPJJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTF4Lk[yOkDPxE1? Mm\MV2FPT0WU
EM-2 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDnTWM2OD1zNz6xOFMh|ryP MmnNV2FPT0WU
HSC-4 Mn\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTF5Lk[2NFEh|ryP NXLUS2dPW0GQR1XS
IGROV-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXH4SlRsUUN3ME2xO{44QDNizszN MkHaV2FPT0WU
TE-1 M2njeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17RfWlEPTB;MUeuPVk3QCEQvF2= NFvESGVUSU6JRWK=
LN-405 NIXFWmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjvTWM2OD1zOT65NFc3KM7:TR?= NYXqTlVCW0GQR1XS
MSTO-211H MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnQTWM2OD1{MD6zOVc{KM7:TR?= MVjTRW5ITVJ?
MOLT-4 NEDuZ5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrsSY5{UUN3ME2yNE42PzV7IN88US=> M2HMTnNCVkeHUh?=
RS4-11 MmDLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTkfml4UUN3ME2yNk4yPTZ|IN88US=> MoLsV2FPT0WU
ES3 NIrXSXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHzTWM2OD1{Mj62PVY{KM7:TR?= NYHvZ256W0GQR1XS
SBC-1 NGS0eGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rkemlEPTB;MkOuPFY6PiEQvF2= MUTTRW5ITVJ?
CTV-1 MmGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTJ3LkCxOFkh|ryP NVvuUow4W0GQR1XS
HuP-T3 M1vsVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnL0TWM2OD1{NT60NFA6KM7:TR?= MUHTRW5ITVJ?
HCC2218 NETpZmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTJ3LkW0NFch|ryP NGf6XldUSU6JRWK=
HDLM-2 MoLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPGWW5KSzVyPUK4MlIxOjZizszN MUnTRW5ITVJ?
ABC-1 M4rQXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnP[WtKSzVyPUK5MlY6PzRizszN MWLTRW5ITVJ?
MV-4-11 NELQW49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTJ7LkezNVch|ryP MknVV2FPT0WU
WM-115 NHPMR4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTNyLkOwPVkh|ryP M4LCWnNCVkeHUh?=
SW1990 NHH4[ItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jBSWlEPTB;M{CuN|Mh|ryP MlLzV2FPT0WU
HCC70 M4Hl[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\MXGRKSzVyPUOwMlc{PDZizszN MljPV2FPT0WU
KYSE-520 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGm1O3FKSzVyPUOwMlg5OzlizszN NE\PdlZUSU6JRWK=
JEG-3 NHzw[WlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnlbmlVUUN3ME2zNU4yPjF2IN88US=> MnTlV2FPT0WU
C8166 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofrTWM2OD1|MT6yNlc1KM7:TR?= NIDEVXZUSU6JRWK=
SK-OV-3 MmDIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHN[GhuUUN3ME2zNU43PzV3IN88US=> M3fMWHNCVkeHUh?=
NCI-H526 Ml:0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTN{Lk[4N{DPxE1? M4H6bnNCVkeHUh?=
NKM-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLzTWM2OD1|Mj65OVY5KM7:TR?= NWjFNWRbW0GQR1XS
ECC10 M{PGVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjyfXlKSzVyPUO0Mlc1PDNizszN NH7NNHNUSU6JRWK=
A2780 MmnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{D5fWlEPTB;M{WuN|YxOSEQvF2= NHewcFNUSU6JRWK=
KY821 NWG5fJA2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTN3Lke2PFEh|ryP M1XLe3NCVkeHUh?=
MKN1 MnvtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LaS2lEPTB;M{[uNlE{PyEQvF2= Mn;wV2FPT0WU
EKVX NIK3dVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFi4TYhKSzVyPUO3MlQzOTJizszN M1zYUHNCVkeHUh?=
EW-16 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1:5VGlEPTB;M{iuN|g5PSEQvF2= M2fXPXNCVkeHUh?=
CTB-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLMTWM2OD1|OT63O|g6KM7:TR?= MXfTRW5ITVJ?
COR-L105 MkTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHiTW1EUUN3ME20NE41PzR4IN88US=> NFjPWpFUSU6JRWK=
NCI-SNU-5 MmrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHNbVZKSzVyPUSxMlIxPjlizszN MXHTRW5ITVJ?
Mewo NH\VSHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13TR2lEPTB;NEGuPVg4OSEQvF2= NEizfoxUSU6JRWK=
BCPAP MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nSS2lEPTB;NEOuO|kyPyEQvF2= M13vXHNCVkeHUh?=
KARPAS-45 NYDGe3pZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknyTWM2OD12ND6yO|c3KM7:TR?= Mm\tV2FPT0WU
NCI-H1693 MkfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrRPGp7UUN3ME20Ok43QTh4IN88US=> M1vud3NCVkeHUh?=
H-EMC-SS MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{f5W2lEPTB;NEiuN|IzPCEQvF2= MmPhV2FPT0WU
697 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPpfol3UUN3ME21NE4{PTR3IN88US=> M{HuVHNCVkeHUh?=
KP-N-YS MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELNb3lKSzVyPUWyMlMyPDJizszN NGiySY5USU6JRWK=
NCI-H1304 NIPEfYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zybGlEPTB;NUKuO|AzPCEQvF2= NIP2NGlUSU6JRWK=
NOS-1 MlS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTtTWM2OD13Mj64OVU6KM7:TR?= M2[zXXNCVkeHUh?=
NCI-H2342 M3K1U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDGTWM2OD13Mz6wOVA5KM7:TR?= M1riUHNCVkeHUh?=
KYSE-270 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XPUmlEPTB;NUOuOlM3PCEQvF2= NX;VOYZsW0GQR1XS
LU-135 M1zhZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUKzcot3UUN3ME21OU4yQDV|IN88US=> NGHPUWNUSU6JRWK=
OE33 Ml7NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjzNWc6UUN3ME21OU45OThizszN MVTTRW5ITVJ?
ML-2 M364[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTsbZNXUUN3ME21OU46PDh7IN88US=> M4DrWHNCVkeHUh?=
KMOE-2 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlm0TWM2OD13Nj6yPFk{KM7:TR?= Mn20V2FPT0WU
Daoy M{XNcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\tWJdKSzVyPUW2MlMzODRizszN NFTVOWlUSU6JRWK=
KNS-62 M{\KW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTV5LkCxOFIh|ryP NX\kO255W0GQR1XS
NBsusSR MlKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHOepFKSzVyPUW3MlU4ODVizszN MWTTRW5ITVJ?
UACC-257 MoHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFi0[3JKSzVyPUW4MlYzPjRizszN MoTsV2FPT0WU
LU-139 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTV6LkiyOkDPxE1? NFLxUnpUSU6JRWK=
CAL-85-1 NF;5Z25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nzV2lEPTB;NUiuPFY1OyEQvF2= NIP5ZmxUSU6JRWK=
NCI-H720 NHvNZ2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDXT4RKSzVyPUW4Mlg6PDJizszN NWHibIQ4W0GQR1XS
MLMA MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmiyTWM2OD13OT6wPVEh|ryP MVTTRW5ITVJ?
A3-KAW M1W0WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTV7LkK4NFkh|ryP M1vzTnNCVkeHUh?=
Ramos-2G6-4C10 M2r0[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTV7Lk[yPFch|ryP MVjTRW5ITVJ?
A388 MoDxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTZyLkS0PUDPxE1? MUXTRW5ITVJ?
LAMA-84 NH;5ZlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TJPGlEPTB;NkCuPVkxPSEQvF2= NGiyd5JUSU6JRWK=
GCT M4\acWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrJVmtxUUN3ME22NU4xPzh4IN88US=> MkTqV2FPT0WU
K-562 NX\hcVZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTZzLkWzN|Mh|ryP MnLrV2FPT0WU
NCI-H1666 MmT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHITWM2OD14MT64O|Uh|ryP NYH1emJkW0GQR1XS
NCI-H1993 NV\pTXJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml75TWM2OD14Mz60NFQ{KM7:TR?= NXHSeJNmW0GQR1XS
NCI-H358 NVfIcXhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzafIQ5UUN3ME22OU4xOTJzIN88US=> NUC1R4RwW0GQR1XS
NB6 MoTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTZ3Lkm4PEDPxE1? NVXhcGFEW0GQR1XS
HCE-T M3rjbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVy0WoxPUUN3ME22O{4xPzl6IN88US=> Mk\MV2FPT0WU
DOK M{XKWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nMO2lEPTB;NkeuOFk1QCEQvF2= NFnlWYFUSU6JRWK=
HT-1376 MmnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rHXmlEPTB;NkmuPFMyPCEQvF2= MmrSV2FPT0WU
NEC8 NXewU2tST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjDN21KSzVyPUewMlEzPDNizszN NYfTWmw5W0GQR1XS
G-402 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHTdok4UUN3ME23NE46Ozl3IN88US=> MVHTRW5ITVJ?
GR-ST MlyxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nFemlEPTB;N{GuNVczKM7:TR?= NFjqVoVUSU6JRWK=
QIMR-WIL MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIL3Z2dKSzVyPUexMlQ1OzRizszN M2LmdHNCVkeHUh?=
CHP-212 MlzOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;kNmdKSzVyPUexMlk3PSEQvF2= MmPkV2FPT0WU
KU812 NIW1O|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTCTWM2OD15Mj65O|AzKM7:TR?= MWLTRW5ITVJ?
Becker MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTd|LkG0PFkh|ryP M1;tUnNCVkeHUh?=
ChaGo-K-1 NXfXcJdLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTd2Lke0PFYh|ryP NX:xeIJ[W0GQR1XS
A498 M33nRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzSfYtKSzVyPUe0Mlk{ODhizszN NInmNIdUSU6JRWK=
NCI-H69 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzZbJlEUUN3ME23OU44PjZ|IN88US=> M361N3NCVkeHUh?=
NCI-H209 M4T3NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTd6Lk[xOFch|ryP MXvTRW5ITVJ?
CAL-33 MoLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTd6Lkm5N|kh|ryP NGjGXVhUSU6JRWK=
COLO-680N NYnXTVlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPEUYdKSzVyPUe5MlExODdizszN M33WZ3NCVkeHUh?=
D-283MED MlTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF2zR2ZKSzVyPUe5MlgyOiEQvF2= NUL2NXkyW0GQR1XS
ATN-1 NGHYdm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vtWmlEPTB;OEGuNVE5PyEQvF2= NUXR[IFIW0GQR1XS
NCI-N87 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rLbGlEPTB;OEGuO|I6PiEQvF2= NVniSHJPW0GQR1XS
MHH-NB-11 NG\ER3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnJbGJsUUN3ME24NU45QDR7IN88US=> NIPlUFRUSU6JRWK=
HEL NYXuTGoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LLWWlEPTB;OEKuOFE{PCEQvF2= MoqxV2FPT0WU
NB69 MkTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzJTWM2OD16Mz6wNFM{KM7:TR?= MorhV2FPT0WU
MPP-89 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\BRWlEPTB;OEOuNlU4PSEQvF2= MV;TRW5ITVJ?
COLO-829 M4jWcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jSfGlEPTB;OEWuOFkyOiEQvF2= NH7VR45USU6JRWK=
ONS-76 MoC5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnCTW13UUN3ME24OU44QTB6IN88US=> MlPkV2FPT0WU
EW-3 NGfKfVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTh4LkKwN|Ih|ryP M1riN3NCVkeHUh?=
EW-11 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDGWFFKSzVyPUi2MlQ{OzZizszN NXjtSmdoW0GQR1XS
SW900 Mlj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEf6[WFKSzVyPUi3MlIxPTNizszN NYK4d4l7W0GQR1XS
MOLT-13 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTh5LkKyOFMh|ryP NGX0OFlUSU6JRWK=
HuP-T4 NHz0Z|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGSyN|RKSzVyPUmxMlA1ODVizszN NH23VplUSU6JRWK=
HCC1419 NVHZd|V1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jpeWlEPTB;OUGuOlM4PCEQvF2= NWjJO2VPW0GQR1XS
CAL-72 NVLHOIhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TsUGlEPTB;OUKuNFIyQSEQvF2= NUfMfogxW0GQR1XS
Mo-T M2LZOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXEd4M2UUN3ME25Nk44Pjl5IN88US=> M2HLfnNCVkeHUh?=
OC-314 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHeweotKSzVyPUmyMlg5OjFizszN MWLTRW5ITVJ?
BHT-101 M3fj[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HMfWlEPTB;OUOuNUDPxE1? M{\kTnNCVkeHUh?=
EW-18 NWjT[VdpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnOyTWM2OD17Mz64OFYzKM7:TR?= M{O1VHNCVkeHUh?=
TE-12 NWPXd5NKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLzTWM2OD17ND6zNFU2KM7:TR?= MkTiV2FPT0WU
MDA-MB-361 NG[0SZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fUWGlEPTB;OU[uNFUyPiEQvF2= Mof1V2FPT0WU

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 52 mg/mL (200.57 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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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