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

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製品説明

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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 MljkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjwTWM2OD1{LkG1NFM5KM7:TR?= MmXDV2FPT0WU
L-363 NHXYb2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zQbGlEPTB;Mj65NlIyOiEQvF2= M3vDXXNCVkeHUh?=
JAR MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTJwOUewNFEh|ryP NYjZSFA6W0GQR1XS
EoL-1-cell MmLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrVTWM2OD12LkGwOVE2KM7:TR?= M3nPPXNCVkeHUh?=
BT-549 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTZwMkG4OFkh|ryP NEjFXWxUSU6JRWK=
SK-NEP-1 M3fvfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrGUZRKSzVyPUeuPFk2OTJizszN NWntcpRuW0GQR1XS
BV-173 NFHTZ2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\kTWM2OD16Lk[3OVg2KM7:TR?= MnvGV2FPT0WU
HMV-II MmrnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\hTWZKSzVyPUGwMlAyPzJizszN MkTjV2FPT0WU
HCC1806 NHe0b4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDJTWM2OD1zMT60OFY4KM7:TR?= NVXBSmUzW0GQR1XS
KASUMI-1 MmLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPZWmVKSzVyPUGxMlU4OSEQvF2= M1KzWHNCVkeHUh?=
SK-MEL-28 Ml7oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWr6T5pOUUN3ME2xNU46PzZ2IN88US=> NFuwZWFUSU6JRWK=
RPMI-8226 M3jsVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjsOVdKSzVyPUGyMlYzPDFizszN NXTvZYtWW0GQR1XS
T47D MoH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF34VI9KSzVyPUGzMlIxQTlizszN NGHiUmFUSU6JRWK=
HOP-62 NFq1eoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MluzTWM2OD1zMz60PEDPxE1? NFXuPZpUSU6JRWK=
A2058 M32yVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XoWmlEPTB;MUOuPFE6QSEQvF2= M{L3NXNCVkeHUh?=
SW620 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITIOFdKSzVyPUG0MlI1PzNizszN Mn3CV2FPT0WU
LCLC-103H NH\oSpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTF2LkS4PVIh|ryP NWm0eFNtW0GQR1XS
HAL-01 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTF2LkW3PVYh|ryP NGLFcHZUSU6JRWK=
PANC-08-13 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPrTWM2OD1zND65NVA5KM7:TR?= NWjSenZTW0GQR1XS
COLO-684 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTF3LkO5O|kh|ryP MYrTRW5ITVJ?
DEL NIKw[YZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fjPGlEPTB;MUWuOFk6KM7:TR?= NYDUbI5nW0GQR1XS
K5 M3ruZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTF4LkG0PFYh|ryP NIXEWYJUSU6JRWK=
SK-MEL-24 NWrpdnRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vScGlEPTB;MU[uOFY2OiEQvF2= MXfTRW5ITVJ?
ACN M{\TUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;oVWlEPTB;MU[uOVI6PyEQvF2= MnP6V2FPT0WU
H9 M1\SeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLYTWM2OD1zNj62NlYh|ryP NVHyTJczW0GQR1XS
EM-2 NVvaUnFsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjie3dKSzVyPUG3MlE1OyEQvF2= M3X6XnNCVkeHUh?=
HSC-4 NGPCenFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTF5Lk[2NFEh|ryP MnLHV2FPT0WU
IGROV-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7kdZNKSzVyPUG3Mlc5OyEQvF2= NEHnXoRUSU6JRWK=
TE-1 NH\xVXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXVcVFKSzVyPUG3Mlk6PjhizszN MX3TRW5ITVJ?
LN-405 NGHFNIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTF7LkmwO|Yh|ryP NHrRWHBUSU6JRWK=
MSTO-211H Ml7JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTJyLkO1O|Mh|ryP MVjTRW5ITVJ?
MOLT-4 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LRXmlEPTB;MkCuOVc2QSEQvF2= NU\SOVJbW0GQR1XS
RS4-11 NF6zTVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;BOHJKSzVyPUKyMlE2PjNizszN M1LOdXNCVkeHUh?=
ES3 NX;XTZUyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TCVGlEPTB;MkKuOlk3OyEQvF2= M12ye3NCVkeHUh?=
SBC-1 M4PTb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfuOXRKSzVyPUKzMlg3QTZizszN NWC4cHQ{W0GQR1XS
CTV-1 Mnm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXHTpBRUUN3ME2yOU4xOTR7IN88US=> MoWwV2FPT0WU
HuP-T3 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF[0[oNKSzVyPUK1MlQxODlizszN NHzJRZNUSU6JRWK=
HCC2218 M4nPdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HkXGlEPTB;MkWuOVQxPyEQvF2= MX;TRW5ITVJ?
HDLM-2 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mli1TWM2OD1{OD6yNFI3KM7:TR?= MnX1V2FPT0WU
ABC-1 NYXmb3NNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLKTWM2OD1{OT62PVc1KM7:TR?= NHvuWo5USU6JRWK=
MV-4-11 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGW4OoxKSzVyPUK5Mlc{OTdizszN NGHlPWxUSU6JRWK=
WM-115 MmHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LzT2lEPTB;M{CuN|A6QSEQvF2= NEfv[odUSU6JRWK=
SW1990 NV32OmlDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmGyTWM2OD1|MD6zN{DPxE1? NH3ZdItUSU6JRWK=
HCC70 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXWRXpyUUN3ME2zNE44OzR4IN88US=> NH\uV29USU6JRWK=
KYSE-520 MnzLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;3UIFKSzVyPUOwMlg5OzlizszN MWfTRW5ITVJ?
JEG-3 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnjNpV[UUN3ME2zNU4yPjF2IN88US=> MXXTRW5ITVJ?
C8166 M{G5cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mki0TWM2OD1|MT6yNlc1KM7:TR?= NYfE[nVkW0GQR1XS
SK-OV-3 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEiwfmFKSzVyPUOxMlY4PTVizszN M{LDOHNCVkeHUh?=
NCI-H526 NIHFTZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTN{Lk[4N{DPxE1? M4fGVHNCVkeHUh?=
NKM-1 NFr5dlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPFTWM2OD1|Mj65OVY5KM7:TR?= M3TxTXNCVkeHUh?=
ECC10 M1S4Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rQPGlEPTB;M{SuO|Q1OyEQvF2= MlrzV2FPT0WU
A2780 MnPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTN3LkO2NFEh|ryP MoD0V2FPT0WU
KY821 MkTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\DXFRKSzVyPUO1Mlc3QDFizszN M3THeXNCVkeHUh?=
MKN1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jBR2lEPTB;M{[uNlE{PyEQvF2= MVzTRW5ITVJ?
EKVX MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPZcHl3UUN3ME2zO{41OjF{IN88US=> NITLXJpUSU6JRWK=
EW-16 NUGwSWs{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\STWM2OD1|OD6zPFg2KM7:TR?= MWDTRW5ITVJ?
CTB-1 NHPOOmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTN7Lke3PFkh|ryP NYXhU4hIW0GQR1XS
COR-L105 NX\Tc2s6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXjWmNOUUN3ME20NE41PzR4IN88US=> M3r1SXNCVkeHUh?=
NCI-SNU-5 MkDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrrVlhNUUN3ME20NU4zODZ7IN88US=> NXfpcnp4W0GQR1XS
Mewo NEXTU41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzoTWM2OD12MT65PFcyKM7:TR?= M2\OSHNCVkeHUh?=
BCPAP MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTR|Lke5NVch|ryP M17xeHNCVkeHUh?=
KARPAS-45 M3TIemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXvVZZKSzVyPUS0MlI4PzZizszN Ml\XV2FPT0WU
NCI-H1693 M4TRdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfmfI5KSzVyPUS2MlY6QDZizszN NYCySYNMW0GQR1XS
H-EMC-SS MnjkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4[5WWlEPTB;NEiuN|IzPCEQvF2= MkHTV2FPT0WU
697 M3\3S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\jTWM2OD13MD6zOVQ2KM7:TR?= MmT4V2FPT0WU
KP-N-YS NFPhR4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\MPYJ5UUN3ME21Nk4{OTR{IN88US=> NHPOfIRUSU6JRWK=
NCI-H1304 NIDXWIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4q5cmlEPTB;NUKuO|AzPCEQvF2= MXHTRW5ITVJ?
NOS-1 MlnmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIniOVFKSzVyPUWyMlg2PTlizszN NXnt[oFVW0GQR1XS
NCI-H2342 MlrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PDPWlEPTB;NUOuNFUxQCEQvF2= MWLTRW5ITVJ?
KYSE-270 NIPvZ2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXv1U|ZIUUN3ME21N{43OzZ2IN88US=> NGr1NI5USU6JRWK=
LU-135 NYnZWHZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLkTWM2OD13NT6xPFU{KM7:TR?= NVf6XVM5W0GQR1XS
OE33 NHSzdIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLpTWM2OD13NT64NVgh|ryP M4\USnNCVkeHUh?=
ML-2 Ml3uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fIU2lEPTB;NUWuPVQ5QSEQvF2= NWrnWm8xW0GQR1XS
KMOE-2 NHzsc2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHuTWM2OD13Nj6yPFk{KM7:TR?= NFLXe|lUSU6JRWK=
Daoy NETqWmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2ruPWlEPTB;NU[uN|IxPCEQvF2= MnW2V2FPT0WU
KNS-62 MlLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHRTWM2OD13Nz6wNVQzKM7:TR?= NYPNUW95W0GQR1XS
NBsusSR MlruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGn0WlBKSzVyPUW3MlU4ODVizszN M4nNTHNCVkeHUh?=
UACC-257 NISyc|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XOdGlEPTB;NUiuOlI3PCEQvF2= NHvLN|lUSU6JRWK=
LU-139 NInPOlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\oTWM2OD13OD64NlYh|ryP MojnV2FPT0WU
CAL-85-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXId4ZoUUN3ME21PE45PjR|IN88US=> Mmi4V2FPT0WU
NCI-H720 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHBR5VKSzVyPUW4Mlg6PDJizszN MULTRW5ITVJ?
MLMA MknRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\1ZlRKSzVyPUW5MlA6OSEQvF2= MVfTRW5ITVJ?
A3-KAW NYT0XGdyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37iZWlEPTB;NUmuNlgxQSEQvF2= M2XISnNCVkeHUh?=
Ramos-2G6-4C10 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DDUGlEPTB;NUmuOlI5PyEQvF2= MXjTRW5ITVJ?
A388 M1vZWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTZyLkS0PUDPxE1? NYr6UVZJW0GQR1XS
LAMA-84 NV20dGk6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILIbo1KSzVyPU[wMlk6ODVizszN NYizV4VGW0GQR1XS
GCT MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXSzeWxPUUN3ME22NU4xPzh4IN88US=> NWjyUFdvW0GQR1XS
K-562 NEDCdHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnuzTWM2OD14MT61N|M{KM7:TR?= NFXPXFVUSU6JRWK=
NCI-H1666 MmfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXe1cmZVUUN3ME22NU45PzVizszN M17kcXNCVkeHUh?=
NCI-H1993 NFrVcFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\FTWM2OD14Mz60NFQ{KM7:TR?= NHL1NXdUSU6JRWK=
NCI-H358 NF7rS21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTZ3LkCxNlEh|ryP NXzwdVV6W0GQR1XS
NB6 Ml7NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHyTWM2OD14NT65PFgh|ryP MUfTRW5ITVJ?
HCE-T NHnPW5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PCW2lEPTB;NkeuNFc6QCEQvF2= M4TKOnNCVkeHUh?=
DOK NYP1OmlTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTZ5LkS5OFgh|ryP MlzwV2FPT0WU
HT-1376 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGS3S3NKSzVyPU[5Mlg{OTRizszN MYjTRW5ITVJ?
NEC8 Mn2wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTnTWM2OD15MD6xNlQ{KM7:TR?= MmXSV2FPT0WU
G-402 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zPbWlEPTB;N{CuPVM6PSEQvF2= M4jmcHNCVkeHUh?=
GR-ST M4H2emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTdzLkG3NkDPxE1? M4\E[3NCVkeHUh?=
QIMR-WIL MknxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXWV45KSzVyPUexMlQ1OzRizszN NG\Cb2pUSU6JRWK=
CHP-212 M4\FNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DpOGlEPTB;N{GuPVY2KM7:TR?= M1\UTHNCVkeHUh?=
KU812 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTd{Lkm3NFIh|ryP NWDUb|lRW0GQR1XS
Becker MnnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELmfIhKSzVyPUezMlE1QDlizszN M4T5SHNCVkeHUh?=
ChaGo-K-1 M3;RcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTKWHhlUUN3ME23OE44PDh4IN88US=> NXPwUYcyW0GQR1XS
A498 NX3qRWZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHRS2xmUUN3ME23OE46OzB6IN88US=> NGXae5dUSU6JRWK=
NCI-H69 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\pS2JKSzVyPUe1Mlc3PjNizszN NXvVd2FrW0GQR1XS
NCI-H209 NWHM[XNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\aXmlEPTB;N{iuOlE1PyEQvF2= MUnTRW5ITVJ?
CAL-33 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTd6Lkm5N|kh|ryP NELuPIpUSU6JRWK=
COLO-680N NH;LfVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELYVoFKSzVyPUe5MlExODdizszN M4HOe3NCVkeHUh?=
D-283MED NI\TUGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTd7LkixNkDPxE1? MoHvV2FPT0WU
ATN-1 MknXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRThzLkGxPFch|ryP MkfJV2FPT0WU
NCI-N87 M3[0UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4m3VGlEPTB;OEGuO|I6PiEQvF2= NVS2dIE5W0GQR1XS
MHH-NB-11 NF7jO5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX:zU3JMUUN3ME24NU45QDR7IN88US=> MoOzV2FPT0WU
HEL NF;Lbo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjY[5pKSzVyPUiyMlQyOzRizszN NYradGw6W0GQR1XS
NB69 NYDLWm9XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTh|LkCwN|Mh|ryP MVHTRW5ITVJ?
MPP-89 M1LnOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInGUXNKSzVyPUizMlI2PzVizszN NXm4S2dnW0GQR1XS
COLO-829 MnXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLRTWM2OD16NT60PVEzKM7:TR?= NIq1cIpUSU6JRWK=
ONS-76 Mo[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrmTWM2OD16NT63PVA5KM7:TR?= MUnTRW5ITVJ?
EW-3 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37kT2lEPTB;OE[uNlA{OiEQvF2= NYjmeJdiW0GQR1XS
EW-11 MnjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTh4LkSzN|Yh|ryP MWXTRW5ITVJ?
SW900 MnPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnBNphKSzVyPUi3MlIxPTNizszN NFfOcIRUSU6JRWK=
MOLT-13 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zSNWlEPTB;OEeuNlI1OyEQvF2= NVrydph6W0GQR1XS
HuP-T4 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTlzLkC0NFUh|ryP M1nnTXNCVkeHUh?=
HCC1419 M4rEeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTlzLk[zO|Qh|ryP M133XXNCVkeHUh?=
CAL-72 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MomyTWM2OD17Mj6wNlE6KM7:TR?= MoHOV2FPT0WU
Mo-T NXj1S4VmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWK3[lNoUUN3ME25Nk44Pjl5IN88US=> MVfTRW5ITVJ?
OC-314 NGPw[4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjMTWM2OD17Mj64PFIyKM7:TR?= NGLOfXhUSU6JRWK=
BHT-101 M2G2TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TtPWlEPTB;OUOuNUDPxE1? NFH5d5pUSU6JRWK=
EW-18 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTl|Lki0OlIh|ryP NEnZb5dUSU6JRWK=
TE-12 M3ziVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37nb2lEPTB;OUSuN|A2PSEQvF2= NHPrR3RUSU6JRWK=
MDA-MB-361 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfxS|lKSzVyPUm2MlA2OTZizszN M3;rd3NCVkeHUh?=

... 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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