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

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MSDS

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 NWDzTJBiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DWU2lEPTB;Mj6xOVA{QCEQvF2= NID0[|FUSU6JRWK=
L-363 NXGzRnNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLRPWJYUUN3ME2yMlkzOjF{IN88US=> NUG4TZl4W0GQR1XS
JAR Ml[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTJwOUewNFEh|ryP MU\TRW5ITVJ?
EoL-1-cell M4\JUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TVemlEPTB;ND6xNFUyPSEQvF2= NIXE[pZUSU6JRWK=
BT-549 NYC4OpFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnpR4dzUUN3ME22MlIyQDR7IN88US=> NYnj[VhoW0GQR1XS
SK-NEP-1 M4ToSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPqflFKSzVyPUeuPFk2OTJizszN M3L1UnNCVkeHUh?=
BV-173 MmfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HnfmlEPTB;OD62O|U5PSEQvF2= MWXTRW5ITVJ?
HMV-II MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfFW25ZUUN3ME2xNE4xOTd{IN88US=> NF;afYVUSU6JRWK=
HCC1806 Mm\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW[1VVh[UUN3ME2xNU41PDZ5IN88US=> NUX5c5BzW0GQR1XS
KASUMI-1 MkexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjkXnNVUUN3ME2xNU42PzFizszN MVrTRW5ITVJ?
SK-MEL-28 NVP2OlRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrpblk6UUN3ME2xNU46PzZ2IN88US=> NG\NNFBUSU6JRWK=
RPMI-8226 NGrHSlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTF{Lk[yOFEh|ryP NHjLNnhUSU6JRWK=
T47D NWLNbYR6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmi0TWM2OD1zMz6yNFk6KM7:TR?= NX7G[FhuW0GQR1XS
HOP-62 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLxTWM2OD1zMz60PEDPxE1? M{PQOHNCVkeHUh?=
A2058 Mk\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPtTG5CUUN3ME2xN{45OTl7IN88US=> NV7s[|JSW0GQR1XS
SW620 Mme3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fGOmlEPTB;MUSuNlQ4OyEQvF2= MYLTRW5ITVJ?
LCLC-103H NYO4RlZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTF2LkS4PVIh|ryP NULFfnZJW0GQR1XS
HAL-01 NF\WR49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvYfWJKSzVyPUG0MlU4QTZizszN MUjTRW5ITVJ?
PANC-08-13 M3LCemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPrTWM2OD1zND65NVA5KM7:TR?= NV64OllsW0GQR1XS
COLO-684 M3nO[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2L3fmlEPTB;MUWuN|k4QSEQvF2= M3\XTnNCVkeHUh?=
DEL NILGSXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTF3LkS5PUDPxE1? NX3qPZNqW0GQR1XS
K5 M2rCSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTF4LkG0PFYh|ryP MV3TRW5ITVJ?
SK-MEL-24 NGLB[FVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2[1PGlEPTB;MU[uOFY2OiEQvF2= NEnwZ3NUSU6JRWK=
ACN NWnHXJozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWS5b4hXUUN3ME2xOk42Ojl5IN88US=> M3W4VXNCVkeHUh?=
H9 Ml3lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTF4Lk[yOkDPxE1? M4DObHNCVkeHUh?=
EM-2 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTF5LkG0N{DPxE1? NYDrSnBIW0GQR1XS
HSC-4 M3rqcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTF5Lk[2NFEh|ryP NXnpTJdEW0GQR1XS
IGROV-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfDV405UUN3ME2xO{44QDNizszN M{n3cnNCVkeHUh?=
TE-1 Mln3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTF5Lkm5Olgh|ryP MlzwV2FPT0WU
LN-405 MnfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\rcIk4UUN3ME2xPU46ODd4IN88US=> NFXhRZZUSU6JRWK=
MSTO-211H MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPETWM2OD1{MD6zOVc{KM7:TR?= MojNV2FPT0WU
MOLT-4 M4LHVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\tfFJKSzVyPUKwMlU4PTlizszN NEPQOFJUSU6JRWK=
RS4-11 NHnBNIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XN[2lEPTB;MkKuNVU3OyEQvF2= NVXNWpJjW0GQR1XS
ES3 M2f1e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTJ{Lk[5OlMh|ryP NWjaVFdJW0GQR1XS
SBC-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3lcoxKSzVyPUKzMlg3QTZizszN MnjnV2FPT0WU
CTV-1 NWTrV4I3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTJ3LkCxOFkh|ryP MoH5V2FPT0WU
HuP-T3 MmfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\HW2ZKSzVyPUK1MlQxODlizszN MXPTRW5ITVJ?
HCC2218 MnrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorBTWM2OD1{NT61OFA4KM7:TR?= M2DoVXNCVkeHUh?=
HDLM-2 M33ybGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFr5PGZKSzVyPUK4MlIxOjZizszN MY\TRW5ITVJ?
ABC-1 NIrrZmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTJ7Lk[5O|Qh|ryP NX60eVlnW0GQR1XS
MV-4-11 NV;lXYh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXwTWM2OD1{OT63N|E4KM7:TR?= MnvmV2FPT0WU
WM-115 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmL6TWM2OD1|MD6zNFk6KM7:TR?= MWPTRW5ITVJ?
SW1990 M4PVSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LC[GlEPTB;M{CuN|Mh|ryP MYjTRW5ITVJ?
HCC70 NHznV2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPET3h3UUN3ME2zNE44OzR4IN88US=> MorKV2FPT0WU
KYSE-520 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILzflVKSzVyPUOwMlg5OzlizszN NHTxSFFUSU6JRWK=
JEG-3 M4nTU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIexR5lKSzVyPUOxMlE3OTRizszN NVj3b41XW0GQR1XS
C8166 M1[wVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1y0cGlEPTB;M{GuNlI4PCEQvF2= NGn6S|JUSU6JRWK=
SK-OV-3 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrnTWM2OD1|MT62O|U2KM7:TR?= MULTRW5ITVJ?
NCI-H526 MljZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nP[WlEPTB;M{KuOlg{KM7:TR?= NWry[GJzW0GQR1XS
NKM-1 M1\ERWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTN{Lkm1Olgh|ryP NXr2d5hSW0GQR1XS
ECC10 NGjJN3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHDbZZKSzVyPUO0Mlc1PDNizszN NWPFU29pW0GQR1XS
A2780 NHjvbXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTN3LkO2NFEh|ryP M{HOcXNCVkeHUh?=
KY821 Mnv4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnW1TWM2OD1|NT63OlgyKM7:TR?= MnvxV2FPT0WU
MKN1 NE\LXJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTwTWM2OD1|Nj6yNVM4KM7:TR?= NHTSN|ZUSU6JRWK=
EKVX M{jkWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTEXlZPUUN3ME2zO{41OjF{IN88US=> NFTzVWRUSU6JRWK=
EW-16 MojKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrrSGZ6UUN3ME2zPE4{QDh3IN88US=> NHXoeWZUSU6JRWK=
CTB-1 NG\XWI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInxWoVKSzVyPUO5Mlc4QDlizszN MlLEV2FPT0WU
COR-L105 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnHWIZKSzVyPUSwMlQ4PDZizszN NXTCOmk6W0GQR1XS
NCI-SNU-5 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTyTWM2OD12MT6yNFY6KM7:TR?= MXjTRW5ITVJ?
Mewo NX3XPVMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTRzLkm4O|Eh|ryP NHfuVHJUSU6JRWK=
BCPAP M2T6SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTR|Lke5NVch|ryP NWrwRm1CW0GQR1XS
KARPAS-45 NHOyNIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTR2LkK3O|Yh|ryP NGGxcG5USU6JRWK=
NCI-H1693 NET4coFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTR4Lk[5PFYh|ryP NGe5bI5USU6JRWK=
H-EMC-SS NUPGOnZWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TJfmlEPTB;NEiuN|IzPCEQvF2= M4LnUHNCVkeHUh?=
697 NHTGcWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\6TWM2OD13MD6zOVQ2KM7:TR?= MXnTRW5ITVJ?
KP-N-YS MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXJVZpKSzVyPUWyMlMyPDJizszN NYTUR4l{W0GQR1XS
NCI-H1304 M1nFPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrxTWM2OD13Mj63NFI1KM7:TR?= M4Thb3NCVkeHUh?=
NOS-1 NFHDU|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTV{Lki1OVkh|ryP MYPTRW5ITVJ?
NCI-H2342 NYP5SXpjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTV|LkC1NFgh|ryP MXHTRW5ITVJ?
KYSE-270 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLjcXdjUUN3ME21N{43OzZ2IN88US=> MmLwV2FPT0WU
LU-135 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrtXlVkUUN3ME21OU4yQDV|IN88US=> MlnmV2FPT0WU
OE33 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmCyTWM2OD13NT64NVgh|ryP NEHyUphUSU6JRWK=
ML-2 NFPIXpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTV3Lkm0PFkh|ryP NXfEPYFDW0GQR1XS
KMOE-2 M2i0eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHi3bppKSzVyPUW2MlI5QTNizszN NYe1NW5UW0GQR1XS
Daoy MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDz[ZFKSzVyPUW2MlMzODRizszN MVnTRW5ITVJ?
KNS-62 NF;NeItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXiUI11UUN3ME21O{4xOTR{IN88US=> NYPObnZuW0GQR1XS
NBsusSR M1v5Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\uOmNKSzVyPUW3MlU4ODVizszN MWjTRW5ITVJ?
UACC-257 MnPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTnTWM2OD13OD62NlY1KM7:TR?= NV22PJZWW0GQR1XS
LU-139 M1L0bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:wZ2lEPTB;NUiuPFI3KM7:TR?= NFe1UYlUSU6JRWK=
CAL-85-1 M{W5OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDlTWM2OD13OD64OlQ{KM7:TR?= NXjZXpNNW0GQR1XS
NCI-H720 M4TQcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPr[2xXUUN3ME21PE45QTR{IN88US=> MmHOV2FPT0WU
MLMA MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIr0OpRKSzVyPUW5MlA6OSEQvF2= MXrTRW5ITVJ?
A3-KAW NXfQW4NXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojBTWM2OD13OT6yPFA6KM7:TR?= NH75fHZUSU6JRWK=
Ramos-2G6-4C10 NXT0ZWtLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LIeWlEPTB;NUmuOlI5PyEQvF2= MV\TRW5ITVJ?
A388 NGHMdYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfsc5IzUUN3ME22NE41PDlizszN NVPEZ417W0GQR1XS
LAMA-84 MkfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTZyLkm5NFUh|ryP MoDBV2FPT0WU
GCT NEXPcVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTZzLkC3PFYh|ryP Ml7RV2FPT0WU
K-562 NUHuNFlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTZzLkWzN|Mh|ryP M3fQW3NCVkeHUh?=
NCI-H1666 NYTmTWFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTZzLki3OUDPxE1? NH25SoNUSU6JRWK=
NCI-H1993 M1\3Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLLTWM2OD14Mz60NFQ{KM7:TR?= MULTRW5ITVJ?
NCI-H358 Mk[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfsbYE1UUN3ME22OU4xOTJzIN88US=> MmTWV2FPT0WU
NB6 M4XVeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTZ3Lkm4PEDPxE1? NF:5PZJUSU6JRWK=
HCE-T Mkf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFKwRXVKSzVyPU[3MlA4QThizszN MUTTRW5ITVJ?
DOK MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTZ5LkS5OFgh|ryP Mm\YV2FPT0WU
HT-1376 NIC2WGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHBTIFKSzVyPU[5Mlg{OTRizszN M3v2R3NCVkeHUh?=
NEC8 Mon4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;kbIp7UUN3ME23NE4yOjR|IN88US=> M1n2Z3NCVkeHUh?=
G-402 NXrTZlVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nzN2lEPTB;N{CuPVM6PSEQvF2= NHzp[mpUSU6JRWK=
GR-ST Mlr1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTdzLkG3NkDPxE1? NXjOemF6W0GQR1XS
QIMR-WIL NFi2NHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml36TWM2OD15MT60OFM1KM7:TR?= M1rQdnNCVkeHUh?=
CHP-212 MlTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjTTo5PUUN3ME23NU46PjVizszN NGrENHhUSU6JRWK=
KU812 M1LDcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\H[2NVUUN3ME23Nk46PzB{IN88US=> MlPxV2FPT0WU
Becker NWnJTHpqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXQSI1KSzVyPUezMlE1QDlizszN MV7TRW5ITVJ?
ChaGo-K-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYj3eIFJUUN3ME23OE44PDh4IN88US=> NETZXVJUSU6JRWK=
A498 NXOwZVExT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2qwbWlEPTB;N{SuPVMxQCEQvF2= MXXTRW5ITVJ?
NCI-H69 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVP3XZk2UUN3ME23OU44PjZ|IN88US=> MXnTRW5ITVJ?
NCI-H209 NGPXS5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3T0SmlEPTB;N{iuOlE1PyEQvF2= MYnTRW5ITVJ?
CAL-33 NVXaXpJlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXQTWM2OD15OD65PVM6KM7:TR?= M3\IdHNCVkeHUh?=
COLO-680N MkXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;qR21bUUN3ME23PU4yODB5IN88US=> M1rad3NCVkeHUh?=
D-283MED NXvoSG5sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTd7LkixNkDPxE1? NWi2W|dmW0GQR1XS
ATN-1 MlrKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRThzLkGxPFch|ryP M2PSWnNCVkeHUh?=
NCI-N87 MoHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILkXWRKSzVyPUixMlczQTZizszN MorBV2FPT0WU
MHH-NB-11 M1vGR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXWTXl{UUN3ME24NU45QDR7IN88US=> NInjUHBUSU6JRWK=
HEL NIi1So1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDmTI1KSzVyPUiyMlQyOzRizszN MlP4V2FPT0WU
NB69 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojiTWM2OD16Mz6wNFM{KM7:TR?= MWrTRW5ITVJ?
MPP-89 NX\xclNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\ueI9pUUN3ME24N{4zPTd3IN88US=> MXLTRW5ITVJ?
COLO-829 NF\jRZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fZZmlEPTB;OEWuOFkyOiEQvF2= M1;aNnNCVkeHUh?=
ONS-76 NFLTSVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTh3Lke5NFgh|ryP NXX5S3FsW0GQR1XS
EW-3 Mli0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3jTWM2OD16Nj6yNFMzKM7:TR?= MoO1V2FPT0WU
EW-11 Mk\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHOXHlKSzVyPUi2MlQ{OzZizszN Mn7nV2FPT0WU
SW900 NHO4dGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTh5LkKwOVMh|ryP M3nC[HNCVkeHUh?=
MOLT-13 MnPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDjOoVCUUN3ME24O{4zOjR|IN88US=> MorGV2FPT0WU
HuP-T4 NFn2[oZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTlzLkC0NFUh|ryP M1\5fnNCVkeHUh?=
HCC1419 NXPHTpk5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;BdWN4UUN3ME25NU43Ozd2IN88US=> M1\m[HNCVkeHUh?=
CAL-72 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknhTWM2OD17Mj6wNlE6KM7:TR?= MnL1V2FPT0WU
Mo-T NETodZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\zbW9KSzVyPUmyMlc3QTdizszN M2TNNHNCVkeHUh?=
OC-314 NXrGV5FKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorXTWM2OD17Mj64PFIyKM7:TR?= MX\TRW5ITVJ?
BHT-101 NGnGRnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnuSWZPUUN3ME25N{4yKM7:TR?= MX;TRW5ITVJ?
EW-18 M1LsNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFr4XGhKSzVyPUmzMlg1PjJizszN NGLBUlFUSU6JRWK=
TE-12 NWLEUm1RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7pOmxKSzVyPUm0MlMxPTVizszN MV\TRW5ITVJ?
MDA-MB-361 M2jLWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTl4LkC1NVYh|ryP MUjTRW5ITVJ?

... 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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