Cyclopamine 化学構造
分子量: 411.62

高品質保証

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MSDS

製品説明

  • Compare Hedgehog/Smoothened Inhibitors
    Hedgehog/Smoothened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 Cyclopamineは、スムーズにされる(SMO)ものの経路敵対者に合図している特定のハリネズミ(Hh)で、 IC50 が 46 nM。
ターゲット Smoothened (Smo)
IC50 46 nM [1]
In vitro試験 Cyclopamine inhibits the Hedgehog signaling pathway with an IC50 of 46 nM, and blocks the activity of human Smo receptor expressed in CHO-K1 cells in [3H]Hh-Ag binding assay with an IC50 of 280 nM. [1] Cyclopamine significantly inhibits Hedgehog pathway activity in a dose-dependent manner in gut-derived tumor cell lines expressing Patched (PTCH) mRNA, and induces growth inhibition of those tumor cell lines by 75-95% at the concentration of 3 μM, but ineffective towards the colon tumor cells without PTCH mRNA expression, suggesting the effects of Cyclopamine treatment are Hedgehog pathway related rather than generally cytotoxic. [2] By blocking Hedgehog signaling through direct interaction with Smo, Cyclopamine (10 μM) inhibits the proliferation of SMOhigh Cyclopamine-responsive cell lines L3.6sl and Panc 05.04 by 75-80%, and increases the apoptosis by 2.5- to 3.5-fold, without affecting the BxPC3-SMOlow cell line. [3] Cyclopamine treatment significantly decreases of Snail mRNA and increasea E-cadherin transcripts in the E3LZ10.7 cell line. Independent of inhibition of cell growth, Cyclopamine treatment significantly inhibits the invasive phenotype of Hedgehog-dependent L3.6pl cells, causing a >500-fold reduction in the number of transmigrating cells, but not that of the Hedgehog-independent cell line Panc-1. [4]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
OS-RC-2 NFzYXpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFGzPZFKSzVyPUWuPFY3PiEQvF2= MXnTRW5ITVJ?
DOHH-2 M1HGWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTlwM{W2PFkh|ryP MoLvV2FPT0WU
no-10 NEPQcYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DlVmlEPTB;OT65NFM6KM7:TR?= MnniV2FPT0WU
LS-513 M3jYNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTFzLkO1OFch|ryP MWfTRW5ITVJ?
ALL-PO NYnxWXg5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4O1SGlEPTB;MUGuO|c{PCEQvF2= Ml3GV2FPT0WU
8-MG-BA NIPBOHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TnZ2lEPTB;MUOuNVEzOyEQvF2= M{jKVXNCVkeHUh?=
RPMI-8402 MnLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDK[49WUUN3ME2xOU45PTN5IN88US=> MYTTRW5ITVJ?
EoL-1-cell MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPSc4tHUUN3ME2xPE42QTR6IN88US=> NWnBNWs2W0GQR1XS
NALM-6 NWjPUlVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTF7LkCxOlch|ryP M1nlcXNCVkeHUh?=
DEL MkPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDHTWM2OD1{MD6xOFcyKM7:TR?= M2HQcnNCVkeHUh?=
SR MkPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjyfI5KSzVyPUKzMlY4OTVizszN NUHV[ZJjW0GQR1XS
697 NVvQTJNxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPLSpE4UUN3ME2yOk43OTV3IN88US=> NGjoVY5USU6JRWK=
COLO-829 M13F[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIruTmpKSzVyPUK2Mlg1QDNizszN M3j3c3NCVkeHUh?=
EVSA-T MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7YRXFKSzVyPUK3MlU2PjFizszN MYXTRW5ITVJ?
ATN-1 MnTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PzfGlEPTB;M{GuNlMzQSEQvF2= MnvRV2FPT0WU
L-363 MkewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzRTWM2OD1|MT63OFYyKM7:TR?= NVTMR5Q2W0GQR1XS
LAMA-84 NF:5dJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jVbGlEPTB;M{KuOVIyOSEQvF2= NWD4fHFEW0GQR1XS
NOS-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjJclVKSzVyPUO0MlI6PTZizszN Mk[3V2FPT0WU
BB30-HNC MlPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHwNZpKSzVyPUO0MlM{ODZizszN M1mxTnNCVkeHUh?=
BC-1 NHP1RoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzITWM2OD1|Nz65O|Q3KM7:TR?= M1Pa[XNCVkeHUh?=
IST-SL2 MkLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjUN2l[UUN3ME2zPE4zOjRizszN NYrZWIdxW0GQR1XS
D-392MG NYjzT4FST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTRyLkKyNVUh|ryP NIq0S5VUSU6JRWK=
no-11 NYO0S21QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoL1TWM2OD12MD61OVIyKM7:TR?= NITu[FNUSU6JRWK=
LC4-1 MlnQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTRyLki3NVYh|ryP NHTMOZJUSU6JRWK=
A388 Ml7DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjjXFBRUUN3ME20Nk42QDR6IN88US=> MkPGV2FPT0WU
NTERA-S-cl-D1 NIDFbmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjOTWM2OD12Mj63NFc1KM7:TR?= NWHGPIlEW0GQR1XS
CESS MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmGxTWM2OD12ND6yNlMzKM7:TR?= MnKxV2FPT0WU
RS4-11 M365cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHKeVlZUUN3ME20PU4xQTN6IN88US=> MVPTRW5ITVJ?
MS-1 NWDnbVd5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIf0OY5KSzVyPUWwMlk{PTFizszN NY\SXZZZW0GQR1XS
CTV-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVm1eJdLUUN3ME21NU4xPzRizszN NYfM[VZLW0GQR1XS
D-502MG NFTafIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPmPHRKSzVyPUWxMlYzPzFizszN NF\R[XFUSU6JRWK=
ML-2 NX7NWFdlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13rbmlEPTB;NUKuPVE6PSEQvF2= NFfySHdUSU6JRWK=
SK-NEP-1 NGjtbGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTrTZBKSzVyPUWzMlM6OjNizszN NHG0cItUSU6JRWK=
LOXIMVI NXnJdodDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHMdFg3UUN3ME21N{42QDh2IN88US=> NV7rPJRDW0GQR1XS
DJM-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHkTWM2OD13Nj6zN|kyKM7:TR?= MmrWV2FPT0WU
GI-1 NHPkPXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkSyTWM2OD13Nj62NVQ6KM7:TR?= NHPieo1USU6JRWK=
IST-MES1 NIfRTFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLWS5NKSzVyPU[wMlU1QTNizszN M1zpc3NCVkeHUh?=
MV-4-11 M3O2RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUX4U4huUUN3ME22NE43PTN6IN88US=> MXfTRW5ITVJ?
OVCAR-4 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXKTWM2OD14Mz61OlU4KM7:TR?= NHm3[YFUSU6JRWK=
KE-37 NVTafGk5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTZ4LkK2Olgh|ryP NGDob5BUSU6JRWK=
D-542MG Ml\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXOxXG5yUUN3ME22PE41OTN3IN88US=> NVzEeZEzW0GQR1XS
MHH-PREB-1 NHewZoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTd{Lki0OFEh|ryP NInrT5VUSU6JRWK=
MRK-nu-1 NFPEc4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37HXmlEPTB;N{OuOFcxPSEQvF2= M3HkS3NCVkeHUh?=
D-247MG MlvNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvPW5dKSzVyPUezMlU1PDJizszN Mn7GV2FPT0WU
OCI-AML2 NGLYSWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnpTWM2OD15Nj65N|Y6KM7:TR?= MnX3V2FPT0WU
LP-1 NYezfllOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXPZWxUUUN3ME24Nk45PzNzIN88US=> M4TTb3NCVkeHUh?=
HCC1599 NF\UZ|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPWTWM2OD16ND6yPFM4KM7:TR?= NIDG[VhUSU6JRWK=
KARPAS-45 NXHsSlF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rMWGlEPTB;OESuOlk6OiEQvF2= NIjROGlUSU6JRWK=
BE-13 NX2y[5JZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoriTWM2OD17OT6wOFc4KM7:TR?= NWDyRXNKW0GQR1XS
GCIY NGTCc2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnJcmVmUUN3ME25PU4xQTV2IN88US=> NGL4ZVJUSU6JRWK=
BV-173 MkTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\XTWM2OD1zMECuN|I2KM7:TR?= MoHGV2FPT0WU
LB2518-MEL MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3y1O2lEPTB;MUCwMlc5QSEQvF2= MVTTRW5ITVJ?
KS-1 NEXvU25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XK[GlEPTB;MUCxMlY{QSEQvF2= NXjZbGRxW0GQR1XS
MOLT-16 M{jyWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTFyND65PFYh|ryP NHrheJRUSU6JRWK=
NCI-H1770 NY\mOlc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfiW3VKSzVyPUGwPE44QDRizszN MlSzV2FPT0WU
NCI-H82 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nuVmlEPTB;MUGwMlk4PiEQvF2= NVj4TplFW0GQR1XS
NCCIT NGjITINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHpbIo5UUN3ME2xNVIvPTJ7IN88US=> NVzr[3JoW0GQR1XS
KALS-1 M1XHTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTFzNT65OFEh|ryP NGnWbmJUSU6JRWK=
LB2241-RCC MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTFzNj62O|kh|ryP MVPTRW5ITVJ?
HH MmTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fWTmlEPTB;MUG3MlM6PSEQvF2= MkfaV2FPT0WU
HD-MY-Z MnjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DBOWlEPTB;MUG4MlQ5QCEQvF2= M3nHXnNCVkeHUh?=
EB-3 NHzUOGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnpVpE2UUN3ME2xNlMvODl2IN88US=> Mn3RV2FPT0WU
BL-70 Mmq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTF{Mz6xNlch|ryP MYPTRW5ITVJ?
K-562 Mn3kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnm0TWM2OD1zMk[uNlQ2KM7:TR?= NH\h[4dUSU6JRWK=
HT-144 NUe0dGU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTF|Mz6xOlQh|ryP NEPRdnNUSU6JRWK=
PF-382 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TFPWlEPTB;MUO0MlM3OSEQvF2= MYHTRW5ITVJ?
RPMI-8226 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDSTIxKSzVyPUGzOU4xPDVizszN NXni[Y1LW0GQR1XS
NCI-H1355 NGO5UXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzMT5JKSzVyPUGzOU42QDdizszN M4joT3NCVkeHUh?=
LXF-289 NV3G[mxxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPrXllKSzVyPUGzPU44QDFizszN MnrxV2FPT0WU
NCI-H69 NGLkU3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mne0TWM2OD1zNEKuPVMzKM7:TR?= NWG2PG5zW0GQR1XS
SK-MEL-1 M1TsNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUi0RYhLUUN3ME2xOFcvOTNizszN MXLTRW5ITVJ?
KARPAS-299 NELDN|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoS0TWM2OD1zNEmuNVIh|ryP M{jIVHNCVkeHUh?=
GB-1 NWruemxrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PyO2lEPTB;MUS5MlMzOiEQvF2= M4jG[3NCVkeHUh?=
CMK MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTF2OT61NVUh|ryP M{DXOnNCVkeHUh?=
MPP-89 MlfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXDZ5JKSzVyPUG1Ok4xOzVizszN MYLTRW5ITVJ?
KU812 NGq5[VlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrSbGJZUUN3ME2xOlEvQTB{IN88US=> M1e1RXNCVkeHUh?=
REH MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUC4dGQ2UUN3ME2xOlIvOTJ3IN88US=> MmC3V2FPT0WU
NEC8 NILQb|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fae2lEPTB;MU[1MlAzPiEQvF2= NFXEbZBUSU6JRWK=
KP-N-YS M2rWb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXMTWM2OD1zNkiuN|k2KM7:TR?= NWTmR5g{W0GQR1XS
Ramos-2G6-4C10 NXTie2dyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTF4OT65NVUh|ryP MUHTRW5ITVJ?
Becker NXzyNIdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;qZmlEPTB;MUe0MlE5KM7:TR?= MYfTRW5ITVJ?
LB647-SCLC MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvwU|JKSzVyPUG3OU45PDVizszN MWHTRW5ITVJ?
LU-139 NFv3bZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTIWnVKSzVyPUG3PE4xOTlizszN M4CwfHNCVkeHUh?=
QIMR-WIL NVjhNXJwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGKxcIRKSzVyPUG3PU43PDZizszN MVzTRW5ITVJ?
NCI-H1395 NWroV4pUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mle0TWM2OD1zN{muPVk3KM7:TR?= NYW2bohmW0GQR1XS
NOMO-1 MmnzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIH5XlNKSzVyPUG4Nk45PSEQvF2= M2DRSHNCVkeHUh?=
GI-ME-N MmHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTF6Nz65Olkh|ryP NEHnWHVUSU6JRWK=
KMS-12-PE MnXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HxTGlEPTB;MUi5MlI4OyEQvF2= NIH5XFdUSU6JRWK=
Daudi Ml;QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fqOGlEPTB;MUmxMlEzQCEQvF2= Ml;SV2FPT0WU
LB996-RCC M4jhRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rqemlEPTB;MUmxMlY6QSEQvF2= MnvuV2FPT0WU
NCI-H2107 MojDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4L5WWlEPTB;MUmzMlc{QSEQvF2= MUTTRW5ITVJ?
SK-PN-DW M2LNN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmO3TWM2OD1zOUSuO|E6KM7:TR?= NFPYNlhUSU6JRWK=
MC-CAR MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTle|dwUUN3ME2yNFIvOjV|IN88US=> NGfUN5lUSU6JRWK=
SNB75 NH3GNZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;3TWM2OD1{MkGuPVQh|ryP MWLTRW5ITVJ?
ES4 Mni4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTJ{Mz63PFMh|ryP NIPndlRUSU6JRWK=
KARPAS-422 NGTD[VFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLRTWM2OD1{MkiuN|UzKM7:TR?= MWnTRW5ITVJ?
NCI-H1648 M2\icWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTJ{OT60PFkh|ryP MknsV2FPT0WU
ES6 NWTxZXpmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{OxNmlEPTB;MkO5MlQ{KM7:TR?= NYLBXnFlW0GQR1XS
KNS-81-FD M{PnTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTJ2MT6xPVch|ryP MoO4V2FPT0WU
JAR NGjEc2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{j4[WlEPTB;MkW2MlIzPSEQvF2= MmHJV2FPT0WU
NB1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHq3Wo9KSzVyPUK2NE42OTZizszN MX3TRW5ITVJ?
D-336MG NUjt[oZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7YZnZ7UUN3ME2yOlAvPjl6IN88US=> NEDHZ25USU6JRWK=
BC-3 NHH1flBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3q2RWlEPTB;Mk[1MlE4QCEQvF2= M123[XNCVkeHUh?=
HCC2218 MnqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTJ4Nj60NVUh|ryP MYDTRW5ITVJ?
TE-9 NGq5ZYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTKTWM2OD1{Nk[uOlI4KM7:TR?= NFfzTm1USU6JRWK=
LB1047-RCC MoPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojaTWM2OD1{Nk[uO|U{KM7:TR?= NUPwbmM3W0GQR1XS
CTB-1 NF3UZ|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfqTWM2OD1{NkmuPVc{KM7:TR?= MV3TRW5ITVJ?
NB7 NWP0[GxHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTJ5MTFOwG0> NV65RVZiW0GQR1XS
ST486 NH22NW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTJ5Nz60NVIh|ryP MX3TRW5ITVJ?
HCC1187 MmXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEj0[VhKSzVyPUK4Nk45OTFizszN MVTTRW5ITVJ?
NCI-SNU-16 Mny1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTJ6ND6yOFgh|ryP MVTTRW5ITVJ?
COR-L279 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\EdFhKSzVyPUK5NU42QDRizszN NIfy[5JUSU6JRWK=
ES8 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTJ7ND6xPFIh|ryP M{nKUXNCVkeHUh?=
U-698-M MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHMTWM2OD1{OUiuNlQ{KM7:TR?= NGfVXFlUSU6JRWK=
HEL NEPSXHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;ONGlEPTB;M{C5MlE1QSEQvF2= MlHXV2FPT0WU
KINGS-1 M4fYPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTNzMD62O|Qh|ryP MmmxV2FPT0WU
KY821 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGX2eodKSzVyPUOzOk42QTVizszN NH7XSnFUSU6JRWK=
MZ1-PC MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHBS4QyUUN3ME2zOFUvPjF6IN88US=> NWfKNVNTW0GQR1XS
LS-411N Ml7tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorpTWM2OD1|NUSuOlYh|ryP M2rU[3NCVkeHUh?=
SIG-M5 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rUR2lEPTB;M{W5Mlc5OiEQvF2= NF\3fnpUSU6JRWK=
HT MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PGTmlEPTB;M{[3MlcyOSEQvF2= NX32d5JtW0GQR1XS
HC-1 M1X0WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTN4Nz63PFch|ryP NVPsNZROW0GQR1XS
NCI-H1694 M4fsdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLHTWM2OD1|N{KuPVM1KM7:TR?= MV3TRW5ITVJ?
BB65-RCC M3n0RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnNPYJKSzVyPUO3Ok4zPDVizszN NELzdmpUSU6JRWK=
HAL-01 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{ewdGlEPTB;M{e5Mlg{QCEQvF2= NHjIclBUSU6JRWK=
ARH-77 NYnHdHdST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknjTWM2OD1|OUSuNFA5KM7:TR?= M1S5[3NCVkeHUh?=
MZ7-mel NFjad5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFL5TGlKSzVyPUO5O{4zOzNizszN M1v3OXNCVkeHUh?=
SIMA NWDpcZhWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnsWXM{UUN3ME20NFMvQTN|IN88US=> NUjxcmtQW0GQR1XS
DG-75 NFvDcY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3W4OmlEPTB;NEG1MlY6QCEQvF2= Mli5V2FPT0WU
HUTU-80 MkP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTRzOT6xPFUh|ryP NYWzXoNxW0GQR1XS
KNS-42 MorDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3ydJNSUUN3ME20NlUvQDF3IN88US=> NHi1ZlRUSU6JRWK=
SH-4 NWLaZpI2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XuZ2lEPTB;NEK3MlU3PSEQvF2= Mn7zV2FPT0WU
L-540 MonIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkKyTWM2OD12M{GuNFMyKM7:TR?= Mkn3V2FPT0WU
NB10 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfpcWJKSzVyPUS0NU4zOzRizszN NHX3N2pUSU6JRWK=
ES1 MnraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPxTWM2OD12NUKuO|U{KM7:TR?= MVTTRW5ITVJ?
KMOE-2 MnztS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3r3eWlEPTB;NEW2MlcyOSEQvF2= M33t[XNCVkeHUh?=
MC116 NIDpSHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGr3SmRKSzVyPUS1PE4yOTZizszN MnfMV2FPT0WU
RCC10RGB NFz2UY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{KxWmlEPTB;NE[wMlAxPSEQvF2= MVrTRW5ITVJ?
RL95-2 MorNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVP5cJhOUUN3ME20OlAvOjN5IN88US=> MkH6V2FPT0WU
Raji MkK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvITWM2OD12NkiuNVQ{KM7:TR?= MYjTRW5ITVJ?
CAS-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TEUWlEPTB;NEeyMlA4OyEQvF2= M{mwTnNCVkeHUh?=
Calu-6 NFrnb2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTR5NT6yOlUh|ryP NWS5OmNUW0GQR1XS
KG-1 M2HJd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PyNmlEPTB;NEe4MlQ1KM7:TR?= M{T6eXNCVkeHUh?=
LB771-HNC NGfUOoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3X6Z2lEPTB;NEiyMlI{OiEQvF2= NIX6c5JUSU6JRWK=
ACN MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTUPJY1UUN3ME20PVMvPTl7IN88US=> NFLYbYxUSU6JRWK=
KM12 NFnGb3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXZclNKSzVyPUS5Ok42QDlizszN MkGyV2FPT0WU

... Click to View More Cell Line Experimental Data

In vivo試験 Administration of Cyclopamine at dose of 50 mg/kg/day for 22 days eradicates the HUCCT1 xenografts in mice with no obvious adverse effects. [2] Cyclopamine treatment at dose of 1.2 mg for 7 days induces significant apoptosis of tumor cells and decreases the tumor mass by 50-60% in Panc 05.04- and L3.6sl-derived tumors, respectively, but not in the BxPC3-SMOlow tumors. [3] Administration of Cyclopamine alone profoundly inhibits tumor metastases in xenografts of E3LZ10.7 and L3.6pl, and completely abrogates metastases when in combination of gemcitabine. [4]
臨床試験
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

Hedgehog cell assay This assay measures the end stage of the Hh signaling pathway, that is, the transcriptional modulation of Gli, using Luciferase as readout (Gli-Luc assay). Cyclopamine is prepared for assay by serial dilution in DMSO and then added to empty assay plates. TM3Hh12 cells (TM3 cells containing Hh-responsive reporter gene construct pTA-8xGli-Luc) are resuspended in F12 Ham's/DMEM (1:1) containing 5% FBS and 15 mM Hepes pH 7.3, added to assay plates and incubated with Cyclopamine for approximately 30 minutes at 37 °C in 5% CO2. 1 nM Hh-Ag 1.5 is then added to assay plates and incubated at 37 °C in the presence of 5% CO2. After 48 hours, either Bright-Glo or MTS reagent is added to the assay plates and luminescence or absorbance at 492 nm is determined. IC50 value, defined as the inflection point of the logistic curve, is determined by non-linear regression of the Gli-driven luciferase luminescence or absorbance signal from MTS assay vs log10 (concentration) of Cyclopamine using the R statistical software pack

細胞アッセイ: [2]

細胞株 SEG1, OE33, KYAE, KYSE180, SNU1, AGS, SNU16, NCI-N-87, HUCCT1, PANC1, PL5, PL6, BXPC3, HS766T, KYSE150, GBD1, DLD1, and HCT116
濃度 Dissolved in DMSO, final concentration 3 μM
反応時間 4 days
実験の流れ Cells are exposed to Cyclopamine in 96-well plates. Cell viability is measured by MTS (soluble tetrazolium salt) assay. Viable cell mass is determined by optical density measurements at 490 nm (OD490) at 2 and 4 days using the CellTiter96 colorimetric assay. Relative growth is calculated as OD (day 4)﹣OD (day 2)/OD (day 2).

動物実験: [2]

動物モデル Athymic (nude) mice inoculated subcutaneously with HUCCT1 cells
製剤 Dissolved in DMSO, and diluted in saline
投薬量 50 mg/kg/day
投与方法 Subcutaneous injection

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 Cyclopamine SDF
分子量 411.62
化学式

C27H41NO2

CAS No. 4449-51-8
保管 3年-20℃
2年-80℃in solvent
別名 11-deoxojervine
溶解度 (25°C) * In vitro DMF 10 mg/mL warming (24.29 mM)
Ethanol 2 mg/mL warming (4.85 mM)
DMSO <1 mg/mL
In vivo 10% DMSO+30% PEG 300+5% Tween 80+ddH2O 1mg/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 Spiro[9H-benzo[a]fluorene-9,2'(3'H)-furo[3,2-b]pyridin]-3-ol, 1,2,3,3'a,4,4',5',6,6',6a,6b,7,7',7'a,8,11,11a,11b-octadecahydro-3',6',10,11b-tetramethyl-, (2'R,3S,3'R,3'aS,6'S,6aS,6bS,7'aR,11aS,11bR)-

文献中の引用 (15)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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