Lenalidomide (CC-5013)

Lenalidomide (CC-5013)は一種のTNF-α分泌阻害剤で、PBMCsの中にIC50値が13 nMです。

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

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製品説明

  • Compare TNF-alpha Inhibitors
    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)は一種のTNF-α分泌阻害剤で、PBMCsの中にIC50値が13 nM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 NHPOfY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXBeYdKSzVyPUKuNVUxOzhizszN NWnCT21CW0GQR1XS
L-363 M1\sfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjJTWM2OD1{LkmyNlEzKM7:TR?= MVfTRW5ITVJ?
JAR NWrHZ2V1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2j5OmlEPTB;Mj65O|AxOSEQvF2= MVnTRW5ITVJ?
EoL-1-cell NYTHdHZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYCxS293UUN3ME20MlExPTF3IN88US=> NGftZ25USU6JRWK=
BT-549 NWiyc413T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrjSGpKSzVyPU[uNlE5PDlizszN MXPTRW5ITVJ?
SK-NEP-1 NXv6UmJST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3G1OWlEPTB;Nz64PVUyOiEQvF2= NWDDcFI{W0GQR1XS
BV-173 M2Gzb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjwTWM2OD16Lk[3OVg2KM7:TR?= NHzyVZNUSU6JRWK=
HMV-II MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1j2OWlEPTB;MUCuNFE4OiEQvF2= MUnTRW5ITVJ?
HCC1806 NHvydI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEL5dHVKSzVyPUGxMlQ1PjdizszN Mnm0V2FPT0WU
KASUMI-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTFzLkW3NUDPxE1? MlS4V2FPT0WU
SK-MEL-28 NF7uPYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvPTWM2OD1zMT65O|Y1KM7:TR?= NXjXNpdpW0GQR1XS
RPMI-8226 M17kNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4i0RmlEPTB;MUKuOlI1OSEQvF2= NEfRXlRUSU6JRWK=
T47D NEHlR5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTF|LkKwPVkh|ryP Moe4V2FPT0WU
HOP-62 NIHZVpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEH4elZKSzVyPUGzMlQ5KM7:TR?= MXfTRW5ITVJ?
A2058 M3zsbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XnXGlEPTB;MUOuPFE6QSEQvF2= MnPyV2FPT0WU
SW620 NH3YU4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17KTGlEPTB;MUSuNlQ4OyEQvF2= NXKzNnVwW0GQR1XS
LCLC-103H MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfTTnNYUUN3ME2xOE41QDl{IN88US=> MmTWV2FPT0WU
HAL-01 M4e5b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfUN5loUUN3ME2xOE42Pzl4IN88US=> NUDOc3dbW0GQR1XS
PANC-08-13 M2noeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zjVGlEPTB;MUSuPVExQCEQvF2= MXzTRW5ITVJ?
COLO-684 NWP1eXVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTF3LkO5O|kh|ryP Mor0V2FPT0WU
DEL NIW1R2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3Ll[WlEPTB;MUWuOFk6KM7:TR?= NWnIc3R6W0GQR1XS
K5 MofyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHX3VJBKSzVyPUG2MlE1QDZizszN NVS2UYlYW0GQR1XS
SK-MEL-24 NYHifo9IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fiWmlEPTB;MU[uOFY2OiEQvF2= NU\CVFBiW0GQR1XS
ACN MoCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHMTWM2OD1zNj61Nlk4KM7:TR?= M2D0UHNCVkeHUh?=
H9 M2XGXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIe3boxKSzVyPUG2MlYzPiEQvF2= M{C5T3NCVkeHUh?=
EM-2 NH;ydYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUG5Umd6UUN3ME2xO{4yPDNizszN NV3rPVZ6W0GQR1XS
HSC-4 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHMTWM2OD1zNz62OlAyKM7:TR?= M1:4NHNCVkeHUh?=
IGROV-1 NHiwfJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{W1fWlEPTB;MUeuO|g{KM7:TR?= NH2zZpdUSU6JRWK=
TE-1 NV3xW4ZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrNTWM2OD1zNz65PVY5KM7:TR?= NXe2SHM3W0GQR1XS
LN-405 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGf5RWhKSzVyPUG5MlkxPzZizszN NGfxVo9USU6JRWK=
MSTO-211H NH70PWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTwTWM2OD1{MD6zOVc{KM7:TR?= NVflbJBLW0GQR1XS
MOLT-4 M36yWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn[1TWM2OD1{MD61O|U6KM7:TR?= M3TxcXNCVkeHUh?=
RS4-11 NXvXSZdyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVr2[GF2UUN3ME2yNk4yPTZ|IN88US=> NGPt[HpUSU6JRWK=
ES3 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4npS2lEPTB;MkKuOlk3OyEQvF2= M3\FWHNCVkeHUh?=
SBC-1 NETUS3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHs[mtKSzVyPUKzMlg3QTZizszN NI\mVXNUSU6JRWK=
CTV-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrvd5lKSzVyPUK1MlAyPDlizszN MUfTRW5ITVJ?
HuP-T3 NYS0bmp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fzeGlEPTB;MkWuOFAxQSEQvF2= NWTqflR6W0GQR1XS
HCC2218 MorUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfiVII6UUN3ME2yOU42PDB5IN88US=> MkLKV2FPT0WU
HDLM-2 M2rteGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLnN4lKSzVyPUK4MlIxOjZizszN NYfBUFJxW0GQR1XS
ABC-1 NX3ITXA5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnqxTWM2OD1{OT62PVc1KM7:TR?= MWfTRW5ITVJ?
MV-4-11 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fybmlEPTB;MkmuO|MyPyEQvF2= NGXt[FBUSU6JRWK=
WM-115 NVj6elZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3exbGlEPTB;M{CuN|A6QSEQvF2= NWmxZXY6W0GQR1XS
SW1990 NUP1SG9KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfRcIRKSzVyPUOwMlM{KM7:TR?= M3zxUHNCVkeHUh?=
HCC70 MkX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVP1b5pDUUN3ME2zNE44OzR4IN88US=> NHvvTXFUSU6JRWK=
KYSE-520 M2rDTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\1TmlEPTB;M{CuPFg{QSEQvF2= NGXS[3hUSU6JRWK=
JEG-3 NEDhe|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\oTWM2OD1|MT6xOlE1KM7:TR?= MVzTRW5ITVJ?
C8166 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUSxNYRLUUN3ME2zNU4zOjd2IN88US=> M{PjdnNCVkeHUh?=
SK-OV-3 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vZPWlEPTB;M{GuOlc2PSEQvF2= NGHjRoNUSU6JRWK=
NCI-H526 MoHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXhdFZKSzVyPUOyMlY5OyEQvF2= NULNeIh3W0GQR1XS
NKM-1 MluxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV76dmpoUUN3ME2zNk46PTZ6IN88US=> MWXTRW5ITVJ?
ECC10 NUTlTXNJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHtTWM2OD1|ND63OFQ{KM7:TR?= M1SySHNCVkeHUh?=
A2780 MlrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTzS5FGUUN3ME2zOU4{PjBzIN88US=> NUj6UHcyW0GQR1XS
KY821 NYDXOmdqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3v4UWlEPTB;M{WuO|Y5OSEQvF2= MWDTRW5ITVJ?
MKN1 MkHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTtTWM2OD1|Nj6yNVM4KM7:TR?= NWrlXJE1W0GQR1XS
EKVX MoPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLWXHBRUUN3ME2zO{41OjF{IN88US=> NGXPVZBUSU6JRWK=
EW-16 NH3tZnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\vTWM2OD1|OD6zPFg2KM7:TR?= MmrGV2FPT0WU
CTB-1 NVj5bVByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvhcZFCUUN3ME2zPU44Pzh7IN88US=> MojVV2FPT0WU
COR-L105 NXXpWoRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnrTWM2OD12MD60O|Q3KM7:TR?= NYmySI9PW0GQR1XS
NCI-SNU-5 Mn7iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\2VmlEPTB;NEGuNlA3QSEQvF2= NEnnRo1USU6JRWK=
Mewo M{fZPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTRzLkm4O|Eh|ryP MlPnV2FPT0WU
BCPAP MoHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\XN4ZKSzVyPUSzMlc6OTdizszN NVTtTVhNW0GQR1XS
KARPAS-45 MoPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fuOmlEPTB;NESuNlc4PiEQvF2= Mn3hV2FPT0WU
NCI-H1693 NYXxTnJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTKTWM2OD12Nj62PVg3KM7:TR?= NIXhb4pUSU6JRWK=
H-EMC-SS NIrKUpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nzXmlEPTB;NEiuN|IzPCEQvF2= MkfYV2FPT0WU
697 M2\RU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV2wbI1JUUN3ME21NE4{PTR3IN88US=> NGLodFJUSU6JRWK=
KP-N-YS MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTV{LkOxOFIh|ryP M4fyS3NCVkeHUh?=
NCI-H1304 NH7x[29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzENWlXUUN3ME21Nk44ODJ2IN88US=> NXjW[oI4W0GQR1XS
NOS-1 Mn;OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYruSVRpUUN3ME21Nk45PTV7IN88US=> Mmn2V2FPT0WU
NCI-H2342 NHfoZm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfRWmVKSzVyPUWzMlA2ODhizszN NYPLbpNmW0GQR1XS
KYSE-270 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXn2eYRXUUN3ME21N{43OzZ2IN88US=> MWXTRW5ITVJ?
LU-135 MnjrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTV3LkG4OVMh|ryP NUP2cFlEW0GQR1XS
OE33 MlK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTV3LkixPEDPxE1? NUTy[3pFW0GQR1XS
ML-2 MoX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfuR4xKSzVyPUW1Mlk1QDlizszN MV3TRW5ITVJ?
KMOE-2 NWnwSVh5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrhTWM2OD13Nj6yPFk{KM7:TR?= NY[zPZNPW0GQR1XS
Daoy MnrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zhUWlEPTB;NU[uN|IxPCEQvF2= NU\mdYwyW0GQR1XS
KNS-62 M3\ENWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLCdJlCUUN3ME21O{4xOTR{IN88US=> NWDLbpJ{W0GQR1XS
NBsusSR M2[0OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLCTWM2OD13Nz61O|A2KM7:TR?= NHTCeYtUSU6JRWK=
UACC-257 NVTDcJMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn64TWM2OD13OD62NlY1KM7:TR?= NF63U|RUSU6JRWK=
LU-139 NFXRdY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XFUGlEPTB;NUiuPFI3KM7:TR?= MonNV2FPT0WU
CAL-85-1 NFXsOIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTV6Lki2OFMh|ryP NFP1OGRUSU6JRWK=
NCI-H720 NWjqfGpNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fVVmlEPTB;NUiuPFk1OiEQvF2= MXnTRW5ITVJ?
MLMA NIXGSJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLXUnU{UUN3ME21PU4xQTFizszN MVPTRW5ITVJ?
A3-KAW MmrSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIq1b2xKSzVyPUW5MlI5ODlizszN MWXTRW5ITVJ?
Ramos-2G6-4C10 M{C2PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTV7Lk[yPFch|ryP NYS5RlN6W0GQR1XS
A388 NFXGRndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXWxTGFTUUN3ME22NE41PDlizszN Ml\kV2FPT0WU
LAMA-84 Ml\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rCbGlEPTB;NkCuPVkxPSEQvF2= NIHOWGVUSU6JRWK=
GCT MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnWTWM2OD14MT6wO|g3KM7:TR?= MlX0V2FPT0WU
K-562 NXvYTJpRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTZzLkWzN|Mh|ryP MWfTRW5ITVJ?
NCI-H1666 MnL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTZzLki3OUDPxE1? MYXTRW5ITVJ?
NCI-H1993 MmixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTZ|LkSwOFMh|ryP NXnNSI1OW0GQR1XS
NCI-H358 Mnn0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3y3dWlEPTB;NkWuNFEzOSEQvF2= NEfkc25USU6JRWK=
NB6 M3W2fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fpcWlEPTB;NkWuPVg5KM7:TR?= MorJV2FPT0WU
HCE-T MoDoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHFfY1KSzVyPU[3MlA4QThizszN NFTtRVVUSU6JRWK=
DOK MnLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLUTWM2OD14Nz60PVQ5KM7:TR?= NILhbY9USU6JRWK=
HT-1376 Mn63S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTZ7LkizNVQh|ryP MonHV2FPT0WU
NEC8 NYDhVIliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjnW4JKSzVyPUewMlEzPDNizszN MYHTRW5ITVJ?
G-402 NI\VcYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnpTWM2OD15MD65N|k2KM7:TR?= Ml[1V2FPT0WU
GR-ST M3;Udmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rkbmlEPTB;N{GuNVczKM7:TR?= M1jNSXNCVkeHUh?=
QIMR-WIL MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlz2TWM2OD15MT60OFM1KM7:TR?= MmLRV2FPT0WU
CHP-212 NX[wWFBQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTdzLkm2OUDPxE1? MYHTRW5ITVJ?
KU812 Ml7WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTd{Lkm3NFIh|ryP Mnz1V2FPT0WU
Becker NX7xWXlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzSXpVHUUN3ME23N{4yPDh7IN88US=> M{\RVXNCVkeHUh?=
ChaGo-K-1 NWiyS3VpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkT6TWM2OD15ND63OFg3KM7:TR?= M2LxbXNCVkeHUh?=
A498 M1jkO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVK3WIVnUUN3ME23OE46OzB6IN88US=> MkK0V2FPT0WU
NCI-H69 Mn3tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTd3Lke2OlMh|ryP NYPpc2NrW0GQR1XS
NCI-H209 NVu1bYl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnWTnlxUUN3ME23PE43OTR5IN88US=> MXPTRW5ITVJ?
CAL-33 NEXTW2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHNTWM2OD15OD65PVM6KM7:TR?= NHHuN2RUSU6JRWK=
COLO-680N NHXCbG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTd7LkGwNFch|ryP MnPNV2FPT0WU
D-283MED MmfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTd7LkixNkDPxE1? NWC2eXhrW0GQR1XS
ATN-1 Mlm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLqTWM2OD16MT6xNVg4KM7:TR?= NV;xNms4W0GQR1XS
NCI-N87 NX\UNWFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRThzLkeyPVYh|ryP NUXET3BzW0GQR1XS
MHH-NB-11 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlW1TWM2OD16MT64PFQ6KM7:TR?= MlnNV2FPT0WU
HEL NG\1blVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXFUGZKSzVyPUiyMlQyOzRizszN MnXQV2FPT0WU
NB69 MoH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTh|LkCwN|Mh|ryP M2P3bHNCVkeHUh?=
MPP-89 NEfLfZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;zbGpKSzVyPUizMlI2PzVizszN M{nI[3NCVkeHUh?=
COLO-829 M2WzZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTh3LkS5NVIh|ryP Mn\XV2FPT0WU
ONS-76 MlPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvSRldKSzVyPUi1Mlc6ODhizszN MWDTRW5ITVJ?
EW-3 M2fwZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\EdGlEPTB;OE[uNlA{OiEQvF2= MmDZV2FPT0WU
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SW900 NUi3VnNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;3b2lEPTB;OEeuNlA2OyEQvF2= NYX6bHFzW0GQR1XS
MOLT-13 MlmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;OTWM2OD16Nz6yNlQ{KM7:TR?= Mmm0V2FPT0WU
HuP-T4 NU\0SY9MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTlzLkC0NFUh|ryP NVnrOYtGW0GQR1XS
HCC1419 Mn3yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\0TWM2OD17MT62N|c1KM7:TR?= MWrTRW5ITVJ?
CAL-72 NV;p[5VpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3LfpFxUUN3ME25Nk4xOjF7IN88US=> NUS2XWVJW0GQR1XS
Mo-T M1fTb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXITWM2OD17Mj63Olk4KM7:TR?= NGTO[GxUSU6JRWK=
OC-314 M2XMemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rxW2lEPTB;OUKuPFgzOSEQvF2= NEf2cVlUSU6JRWK=
BHT-101 M{G4eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXrT3BHUUN3ME25N{4yKM7:TR?= MV\TRW5ITVJ?
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TE-12 NIDSToNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3oTWM2OD17ND6zNFU2KM7:TR?= MoPEV2FPT0WU
MDA-MB-361 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;KbVRIUUN3ME25Ok4xPTF4IN88US=> M2XFW3NCVkeHUh?=

... 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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