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

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MSDS

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 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTXTWM2OD1{LkG1NFM5KM7:TR?= MoPWV2FPT0WU
L-363 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnSzTWM2OD1{LkmyNlEzKM7:TR?= NXrtfllzW0GQR1XS
JAR NXHrWZJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnXfWxKSzVyPUKuPVcxODFizszN NWTiTHB3W0GQR1XS
EoL-1-cell M1TJXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1T1cGlEPTB;ND6xNFUyPSEQvF2= MWrTRW5ITVJ?
BT-549 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTZwMkG4OFkh|ryP M2PZ[HNCVkeHUh?=
SK-NEP-1 NUnaNVhWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU[1TIRWUUN3ME23Mlg6PTF{IN88US=> NXzjeHJGW0GQR1XS
BV-173 NWDIbpdmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHiwNW9KSzVyPUiuOlc2QDVizszN M1e3fnNCVkeHUh?=
HMV-II M13Demdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Lvb2lEPTB;MUCuNFE4OiEQvF2= MXTTRW5ITVJ?
HCC1806 M{jQemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XPVmlEPTB;MUGuOFQ3PyEQvF2= MYDTRW5ITVJ?
KASUMI-1 MmDsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXWW41GUUN3ME2xNU42PzFizszN NUDFdJQ1W0GQR1XS
SK-MEL-28 M4TxN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljCTWM2OD1zMT65O|Y1KM7:TR?= M2fqS3NCVkeHUh?=
RPMI-8226 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTF{Lk[yOFEh|ryP MWPTRW5ITVJ?
T47D M17ibWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXudlNkUUN3ME2xN{4zODl7IN88US=> M1i1R3NCVkeHUh?=
HOP-62 NYPTcpcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moi3TWM2OD1zMz60PEDPxE1? MXXTRW5ITVJ?
A2058 NIHTW2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjMOWtHUUN3ME2xN{45OTl7IN88US=> NEDsVnBUSU6JRWK=
SW620 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHoXo5KSzVyPUG0MlI1PzNizszN MkDEV2FPT0WU
LCLC-103H NW\rSnRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfQTWM2OD1zND60PFkzKM7:TR?= NYPlVJpPW0GQR1XS
HAL-01 NXWwOoRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DWPWlEPTB;MUSuOVc6PiEQvF2= MVnTRW5ITVJ?
PANC-08-13 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\UTmlEPTB;MUSuPVExQCEQvF2= MWjTRW5ITVJ?
COLO-684 NUXUfJRuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTF3LkO5O|kh|ryP MWLTRW5ITVJ?
DEL NGi1W45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLYTWM2OD1zNT60PVkh|ryP MlTtV2FPT0WU
K5 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTF4LkG0PFYh|ryP M3fYUnNCVkeHUh?=
SK-MEL-24 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDBcHRiUUN3ME2xOk41PjV{IN88US=> NIGzOWNUSU6JRWK=
ACN NEf0fmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTF4LkWyPVch|ryP M1XwUXNCVkeHUh?=
H9 NEXRVohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTF4Lk[yOkDPxE1? M4DocnNCVkeHUh?=
EM-2 MmHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTF5LkG0N{DPxE1? NXrjdFNZW0GQR1XS
HSC-4 M1X2W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHaTWM2OD1zNz62OlAyKM7:TR?= M3qyb3NCVkeHUh?=
IGROV-1 M3HRfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYCwbldmUUN3ME2xO{44QDNizszN M3;3W3NCVkeHUh?=
TE-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrCO5BKSzVyPUG3Mlk6PjhizszN NILkRVhUSU6JRWK=
LN-405 M3;KT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTF7LkmwO|Yh|ryP NFLsc|ZUSU6JRWK=
MSTO-211H M3Pjb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XhTGlEPTB;MkCuN|U4OyEQvF2= NYWzcFA4W0GQR1XS
MOLT-4 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLHTWM2OD1{MD61O|U6KM7:TR?= NYPrcotMW0GQR1XS
RS4-11 M3PYXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGS3WJNKSzVyPUKyMlE2PjNizszN MmfkV2FPT0WU
ES3 NGPmT4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjHNW1nUUN3ME2yNk43QTZ|IN88US=> NUjxSXdlW0GQR1XS
SBC-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYX2N41mUUN3ME2yN{45Pjl4IN88US=> NE\kOllUSU6JRWK=
CTV-1 M2\tbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTBTWM2OD1{NT6wNVQ6KM7:TR?= MmnUV2FPT0WU
HuP-T3 MkS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTJ3LkSwNFkh|ryP NWHL[JNFW0GQR1XS
HCC2218 MlTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LTdWlEPTB;MkWuOVQxPyEQvF2= NUDYRmFDW0GQR1XS
HDLM-2 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTJ6LkKwNlYh|ryP MUTTRW5ITVJ?
ABC-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTJ7Lk[5O|Qh|ryP NYnkTlI5W0GQR1XS
MV-4-11 MmTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTJ7LkezNVch|ryP M2LpZXNCVkeHUh?=
WM-115 MlzyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofxTWM2OD1|MD6zNFk6KM7:TR?= MYPTRW5ITVJ?
SW1990 M4\hc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXuV2ZKSzVyPUOwMlM{KM7:TR?= NHzLWG1USU6JRWK=
HCC70 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGflfI1KSzVyPUOwMlc{PDZizszN NYHJS3RlW0GQR1XS
KYSE-520 M4PpPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4W5bmlEPTB;M{CuPFg{QSEQvF2= M2Tm[XNCVkeHUh?=
JEG-3 NFnjTY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LlXmlEPTB;M{GuNVYyPCEQvF2= MXTTRW5ITVJ?
C8166 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTNzLkKyO|Qh|ryP M4nRVnNCVkeHUh?=
SK-OV-3 M2[3Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\PZmlEPTB;M{GuOlc2PSEQvF2= NYHsTYFkW0GQR1XS
NCI-H526 MnTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTsTWM2OD1|Mj62PFMh|ryP NXSy[G1[W0GQR1XS
NKM-1 NFzM[m5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{[wWmlEPTB;M{KuPVU3QCEQvF2= NHTpXIxUSU6JRWK=
ECC10 MmrtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXriNlFHUUN3ME2zOE44PDR|IN88US=> NGPxbWxUSU6JRWK=
A2780 MoHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XsR2lEPTB;M{WuN|YxOSEQvF2= NWTkNHVGW0GQR1XS
KY821 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDPTWM2OD1|NT63OlgyKM7:TR?= MVvTRW5ITVJ?
MKN1 M33W[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7iTnVKSzVyPUO2MlIyOzdizszN NXP4O2t7W0GQR1XS
EKVX M1LufWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTzTWM2OD1|Nz60NlEzKM7:TR?= NUfMTWxDW0GQR1XS
EW-16 MnLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHRdY5sUUN3ME2zPE4{QDh3IN88US=> M{DsbXNCVkeHUh?=
CTB-1 MlTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHyWoF3UUN3ME2zPU44Pzh7IN88US=> NY\1Om1yW0GQR1XS
COR-L105 M2m4V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlOyTWM2OD12MD60O|Q3KM7:TR?= Mli4V2FPT0WU
NCI-SNU-5 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTRzLkKwOlkh|ryP MXjTRW5ITVJ?
Mewo NELuZ5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3uySmlEPTB;NEGuPVg4OSEQvF2= NFvkXlJUSU6JRWK=
BCPAP NW\XPGtQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXTVYFKSzVyPUSzMlc6OTdizszN MYPTRW5ITVJ?
KARPAS-45 MkGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrkTWM2OD12ND6yO|c3KM7:TR?= NVr4TmJTW0GQR1XS
NCI-H1693 M3XLNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTR4Lk[5PFYh|ryP NEPlNnJUSU6JRWK=
H-EMC-SS M3HQW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFv5dVRKSzVyPUS4MlMzOjRizszN NWT4Um05W0GQR1XS
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KP-N-YS MlzkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\Wd2lEPTB;NUKuN|E1OiEQvF2= NVLXXHE4W0GQR1XS
NCI-H1304 NFHCXpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXITWM2OD13Mj63NFI1KM7:TR?= MX3TRW5ITVJ?
NOS-1 MnO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTV{Lki1OVkh|ryP MnLHV2FPT0WU
NCI-H2342 M4K5[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTV|LkC1NFgh|ryP NFzp[npUSU6JRWK=
KYSE-270 NHHafJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmqyTWM2OD13Mz62N|Y1KM7:TR?= NI\2WW5USU6JRWK=
LU-135 M{\aXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXru[4F4UUN3ME21OU4yQDV|IN88US=> MnPNV2FPT0WU
OE33 Mn;xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGCzbllKSzVyPUW1MlgyQCEQvF2= MYXTRW5ITVJ?
ML-2 NYrrOJVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XaXWlEPTB;NUWuPVQ5QSEQvF2= NUDadoczW0GQR1XS
KMOE-2 M4nHTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLYZ|BQUUN3ME21Ok4zQDl|IN88US=> Mo\sV2FPT0WU
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NBsusSR NFu2SJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Dv[2lEPTB;NUeuOVcxPSEQvF2= MojsV2FPT0WU
UACC-257 NVn5W5RiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3S3cGlEPTB;NUiuOlI3PCEQvF2= M1;1ZnNCVkeHUh?=
LU-139 MnO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHo[WxTUUN3ME21PE45OjZizszN NUTLd|RqW0GQR1XS
CAL-85-1 MnvQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDyTWM2OD13OD64OlQ{KM7:TR?= NGm1dXRUSU6JRWK=
NCI-H720 M4[3R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTV6Lki5OFIh|ryP M2TmbXNCVkeHUh?=
MLMA M3fzTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7QV3F2UUN3ME21PU4xQTFizszN NYLpW5lkW0GQR1XS
A3-KAW MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTV7LkK4NFkh|ryP MkThV2FPT0WU
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LAMA-84 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTZyLkm5NFUh|ryP M4DJRnNCVkeHUh?=
GCT MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfqcotKSzVyPU[xMlA4QDZizszN NX3XTYQxW0GQR1XS
K-562 MoDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfqTYdlUUN3ME22NU42OzN|IN88US=> NX7BbVNKW0GQR1XS
NCI-H1666 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV34WVZLUUN3ME22NU45PzVizszN M{fBc3NCVkeHUh?=
NCI-H1993 MkLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTZ|LkSwOFMh|ryP M{fJPXNCVkeHUh?=
NCI-H358 MlP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTZ3LkCxNlEh|ryP MoK5V2FPT0WU
NB6 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXETWM2OD14NT65PFgh|ryP MoHvV2FPT0WU
HCE-T NEHoPGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDxRYlKSzVyPU[3MlA4QThizszN NYHxdnZtW0GQR1XS
DOK NH7VbYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHofotKSzVyPU[3MlQ6PDhizszN M4fBXXNCVkeHUh?=
HT-1376 MmT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTZ7LkizNVQh|ryP NHrxSJlUSU6JRWK=
NEC8 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\6N2lEPTB;N{CuNVI1OyEQvF2= NXPjdlloW0GQR1XS
G-402 NYXuSFZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrCR5JKSzVyPUewMlk{QTVizszN Mn\uV2FPT0WU
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QIMR-WIL MlvRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWH4XpBUUUN3ME23NU41PDN2IN88US=> MkDLV2FPT0WU
CHP-212 MlezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGSxdoVKSzVyPUexMlk3PSEQvF2= M{L6ZnNCVkeHUh?=
KU812 NYrmcYlKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnYOIZjUUN3ME23Nk46PzB{IN88US=> NGfke3NUSU6JRWK=
Becker NXj6ZYlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTd|LkG0PFkh|ryP M2jFXHNCVkeHUh?=
ChaGo-K-1 NEfRPIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHhUnZKSzVyPUe0Mlc1QDZizszN MWjTRW5ITVJ?
A498 NW\1S|VnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofRTWM2OD15ND65N|A5KM7:TR?= NHrGeoJUSU6JRWK=
NCI-H69 NYLiT|dOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zpN2lEPTB;N{WuO|Y3OyEQvF2= NWPlSFlYW0GQR1XS
NCI-H209 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjvNWJKSzVyPUe4MlYyPDdizszN NVPSOJBJW0GQR1XS
CAL-33 NHvUcndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnS3TWM2OD15OD65PVM6KM7:TR?= NVSwZXZXW0GQR1XS
COLO-680N Mon3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHlTWM2OD15OT6xNFA4KM7:TR?= MX\TRW5ITVJ?
D-283MED NFLUfIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PHbmlEPTB;N{muPFEzKM7:TR?= M2XjdHNCVkeHUh?=
ATN-1 NHG2dW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TpdmlEPTB;OEGuNVE5PyEQvF2= NE\IcmZUSU6JRWK=
NCI-N87 NH\NNWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fwfWlEPTB;OEGuO|I6PiEQvF2= MWHTRW5ITVJ?
MHH-NB-11 M3P5NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUGwN|VFUUN3ME24NU45QDR7IN88US=> NGLiTm1USU6JRWK=
HEL Mme0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTh{LkSxN|Qh|ryP NHvsUmZUSU6JRWK=
NB69 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jBOWlEPTB;OEOuNFA{OyEQvF2= MknIV2FPT0WU
MPP-89 MmTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HibWlEPTB;OEOuNlU4PSEQvF2= Mo\YV2FPT0WU
COLO-829 NUnyZmxVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHYW5VEUUN3ME24OU41QTF{IN88US=> NHXSWnZUSU6JRWK=
ONS-76 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYGyV2ZGUUN3ME24OU44QTB6IN88US=> NYnVeZdJW0GQR1XS
EW-3 M{XSfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mle4TWM2OD16Nj6yNFMzKM7:TR?= Mn;LV2FPT0WU
EW-11 M3zz[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vrZ2lEPTB;OE[uOFM{PiEQvF2= M{fy[3NCVkeHUh?=
SW900 NVHvVlFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DqcmlEPTB;OEeuNlA2OyEQvF2= M1XC[3NCVkeHUh?=
MOLT-13 Mn7BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jMe2lEPTB;OEeuNlI1OyEQvF2= MnL6V2FPT0WU
HuP-T4 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPLTWM2OD17MT6wOFA2KM7:TR?= M3n0O3NCVkeHUh?=
HCC1419 NFXhVZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{X5U2lEPTB;OUGuOlM4PCEQvF2= NFzYNZVUSU6JRWK=
CAL-72 M4H6emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXPVXFKSzVyPUmyMlAzOTlizszN NFnwWVNUSU6JRWK=
Mo-T NWryO3lzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHRTWM2OD17Mj63Olk4KM7:TR?= MYnTRW5ITVJ?
OC-314 MoLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fZcWlEPTB;OUKuPFgzOSEQvF2= NUTU[5hkW0GQR1XS
BHT-101 Ml:1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTl|LkGg{txO NHu3d2VUSU6JRWK=
EW-18 M1ryVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYL6e4ZZUUN3ME25N{45PDZ{IN88US=> NWf0UYtUW0GQR1XS
TE-12 M4rYWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlT2TWM2OD17ND6zNFU2KM7:TR?= Ml\0V2FPT0WU
MDA-MB-361 M{DKWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTl4LkC1NVYh|ryP MormV2FPT0WU

... 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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