Cyclopamine 化学構造
分子量: 411.62

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Quality Control & 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 MoTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjwSpk2UUN3ME21Mlg3PjZizszN MnrYV2FPT0WU
DOHH-2 NUXwbWR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfXTWM2OD17LkO1Olg6KM7:TR?= NY\neWNkW0GQR1XS
no-10 NYDaWY52T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2[4VmlEPTB;OT65NFM6KM7:TR?= NVvxTpl[W0GQR1XS
LS-513 MlrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HjcWlEPTB;MUGuN|U1PyEQvF2= M1TLVXNCVkeHUh?=
ALL-PO NUfOUpppT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fQcWlEPTB;MUGuO|c{PCEQvF2= M2fT[HNCVkeHUh?=
8-MG-BA MlfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvW[5FKSzVyPUGzMlEyOjNizszN MW\TRW5ITVJ?
RPMI-8402 NYHmenBkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXUTWM2OD1zNT64OVM4KM7:TR?= NXiyfWRiW0GQR1XS
EoL-1-cell Mkn6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3uwVGlEPTB;MUiuOVk1QCEQvF2= NXz6PXJLW0GQR1XS
NALM-6 M3PHS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfITWM2OD1zOT6wNVY4KM7:TR?= M{f5OXNCVkeHUh?=
DEL MluxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLEeXJwUUN3ME2yNE4yPDdzIN88US=> MoD3V2FPT0WU
SR MmrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmW5TWM2OD1{Mz62O|E2KM7:TR?= MXrTRW5ITVJ?
697 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojXTWM2OD1{Nj62NVU2KM7:TR?= MnLtV2FPT0WU
COLO-829 NGPxOJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoT5TWM2OD1{Nj64OFg{KM7:TR?= MkLnV2FPT0WU
EVSA-T M3Hl[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nDcWlEPTB;MkeuOVU3OSEQvF2= MVrTRW5ITVJ?
ATN-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7aXFRKSzVyPUOxMlI{OjlizszN NIO2VlZUSU6JRWK=
L-363 M{TRUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmS5TWM2OD1|MT63OFYyKM7:TR?= M{\uXnNCVkeHUh?=
LAMA-84 NGX4OW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\TdJBZUUN3ME2zNk42OjFzIN88US=> NInLdVlUSU6JRWK=
NOS-1 MmrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTN2LkK5OVYh|ryP NHq1XotUSU6JRWK=
BB30-HNC MlvES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPhTWM2OD1|ND6zN|A3KM7:TR?= MlzpV2FPT0WU
BC-1 M{D1Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrj[mg1UUN3ME2zO{46PzR4IN88US=> M4HLdXNCVkeHUh?=
IST-SL2 NHWzc4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HOdWlEPTB;M{iuNlI1KM7:TR?= NFiyVYdUSU6JRWK=
D-392MG MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHRTWM2OD12MD6yNlE2KM7:TR?= NYjG[IZqW0GQR1XS
no-11 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrYfGdvUUN3ME20NE42PTJzIN88US=> M2XtVXNCVkeHUh?=
LC4-1 MlnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTRyLki3NVYh|ryP NGr4dHpUSU6JRWK=
A388 MonNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLiTWM2OD12Mj61PFQ5KM7:TR?= M2XlOHNCVkeHUh?=
NTERA-S-cl-D1 NYPue3NtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTR{LkewO|Qh|ryP MmnMV2FPT0WU
CESS MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17EWGlEPTB;NESuNlI{OiEQvF2= NUn2ZoZ[W0GQR1XS
RS4-11 Ml25S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfM[I9GUUN3ME20PU4xQTN6IN88US=> Mn;IV2FPT0WU
MS-1 NUnjd3BDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHr2eohKSzVyPUWwMlk{PTFizszN NHTpOopUSU6JRWK=
CTV-1 NGnyVplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTVzLkC3OEDPxE1? NYLveHM{W0GQR1XS
D-502MG NV3FcGNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jNWWlEPTB;NUGuOlI4OSEQvF2= Mn\uV2FPT0WU
ML-2 Mnf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7uZnE2UUN3ME21Nk46OTl3IN88US=> NHXZb5dUSU6JRWK=
SK-NEP-1 NFK2VmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TlemlEPTB;NUOuN|kzOyEQvF2= NYizNXJQW0GQR1XS
LOXIMVI MkLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnSzTWM2OD13Mz61PFg1KM7:TR?= M372bnNCVkeHUh?=
DJM-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\IRmlEPTB;NU[uN|M6OSEQvF2= NEDGOoNUSU6JRWK=
GI-1 NF;GRpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXe5eHY5UUN3ME21Ok43OTR7IN88US=> NYf6cXl7W0GQR1XS
IST-MES1 Mm\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TUc2lEPTB;NkCuOVQ6OyEQvF2= NWfIZ5d3W0GQR1XS
MV-4-11 NEDaTWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3jTWM2OD14MD62OVM5KM7:TR?= NVXnc4FDW0GQR1XS
OVCAR-4 NXjxV4gyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\CTWM2OD14Mz61OlU4KM7:TR?= NGrjZ5RUSU6JRWK=
KE-37 NGDZOHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HodmlEPTB;Nk[uNlY3QCEQvF2= NVm0XYU2W0GQR1XS
D-542MG NHXKcFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG[2XIlKSzVyPU[4MlQyOzVizszN M3XqcnNCVkeHUh?=
MHH-PREB-1 NIHJdZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTd{Lki0OFEh|ryP MYfTRW5ITVJ?
MRK-nu-1 NGjK[XpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nsUGlEPTB;N{OuOFcxPSEQvF2= MYPTRW5ITVJ?
D-247MG M4Hpb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDhepJPUUN3ME23N{42PDR{IN88US=> NX3rPG45W0GQR1XS
OCI-AML2 MonjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWn5c|ZEUUN3ME23Ok46OzZ7IN88US=> MomxV2FPT0WU
LP-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHj1TlBKSzVyPUiyMlg4OzFizszN MYrTRW5ITVJ?
HCC1599 NF3aSVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfRTWM2OD16ND6yPFM4KM7:TR?= MonWV2FPT0WU
KARPAS-45 NHvPSFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHUTWM2OD16ND62PVkzKM7:TR?= MlnwV2FPT0WU
BE-13 M1zOb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnr6TWM2OD17OT6wOFc4KM7:TR?= MnzLV2FPT0WU
GCIY NFLHNVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljnTWM2OD17OT6wPVU1KM7:TR?= M2DDZnNCVkeHUh?=
BV-173 MnzIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPxc5lKSzVyPUGwNE4{OjVizszN MY\TRW5ITVJ?
LB2518-MEL MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYf6bHloUUN3ME2xNFAvPzh7IN88US=> MWLTRW5ITVJ?
KS-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3uTWM2OD1zMEGuOlM6KM7:TR?= MoXpV2FPT0WU
MOLT-16 M1;q[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknoTWM2OD1zMESuPVg3KM7:TR?= NXvlRVNoW0GQR1XS
NCI-H1770 NIDJUXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLlTWM2OD1zMEiuO|g1KM7:TR?= NEfDdIhUSU6JRWK=
NCI-H82 NIHTSo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4D4W2lEPTB;MUGwMlk4PiEQvF2= M17CfHNCVkeHUh?=
NCCIT MoG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXoNHFSUUN3ME2xNVIvPTJ7IN88US=> M1zJUHNCVkeHUh?=
KALS-1 MlHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXaTWM2OD1zMUWuPVQyKM7:TR?= NITSOJJUSU6JRWK=
LB2241-RCC NWq1flg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTFzNj62O|kh|ryP MmPrV2FPT0WU
HH M{HvOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2frUGlEPTB;MUG3MlM6PSEQvF2= MUTTRW5ITVJ?
HD-MY-Z MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zRU2lEPTB;MUG4MlQ5QCEQvF2= NWTxOY9UW0GQR1XS
EB-3 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TZOmlEPTB;MUKzMlA6PCEQvF2= M{LNRXNCVkeHUh?=
BL-70 MoS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfZT5BKSzVyPUGyN{4yOjdizszN Moe0V2FPT0WU
K-562 M{fuTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX2zfVlzUUN3ME2xNlYvOjR3IN88US=> M1PWTHNCVkeHUh?=
HT-144 NYjuTYRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LIWWlEPTB;MUOzMlE3PCEQvF2= MWrTRW5ITVJ?
PF-382 MlrjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rjZWlEPTB;MUO0MlM3OSEQvF2= NUG2OHh[W0GQR1XS
RPMI-8226 NYO4XZZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTF|NT6wOFUh|ryP MXLTRW5ITVJ?
NCI-H1355 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPHdYNwUUN3ME2xN|UvPTh5IN88US=> NV3DOG9VW0GQR1XS
LXF-289 NX6zZ|Y3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NED5[IJKSzVyPUGzPU44QDFizszN NXTKTWpMW0GQR1XS
NCI-H69 M{HuXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zie2lEPTB;MUSyMlk{OiEQvF2= M3[xZ3NCVkeHUh?=
SK-MEL-1 NGHOUmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3OyTWlEPTB;MUS3MlE{KM7:TR?= MXrTRW5ITVJ?
KARPAS-299 NVHFfXFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HnPGlEPTB;MUS5MlEzKM7:TR?= MXvTRW5ITVJ?
GB-1 M{HoW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHsTWM2OD1zNEmuN|IzKM7:TR?= NH\xdZlUSU6JRWK=
CMK M1;Td2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnBPFg{UUN3ME2xOFkvPTF3IN88US=> MoXDV2FPT0WU
MPP-89 M1PtRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\XTVRpUUN3ME2xOVYvODN3IN88US=> NYnlUFBsW0GQR1XS
KU812 M33memdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrUWWtKSzVyPUG2NU46ODJizszN NXXSTnVjW0GQR1XS
REH M4jCb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTF4Mj6xNlUh|ryP Mmm0V2FPT0WU
NEC8 NUXmfW9NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTEbGU4UUN3ME2xOlUvODJ4IN88US=> NYPRfXFXW0GQR1XS
KP-N-YS MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\UXGlEPTB;MU[4MlM6PSEQvF2= Mn\hV2FPT0WU
Ramos-2G6-4C10 NFr2cXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTF4OT65NVUh|ryP NGLsVmRUSU6JRWK=
Becker MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTF5ND6xPEDPxE1? M4\l[HNCVkeHUh?=
LB647-SCLC MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnESHlKSzVyPUG3OU45PDVizszN M1HPOHNCVkeHUh?=
LU-139 NFfXbFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvTTWM2OD1zN{iuNFE6KM7:TR?= MYfTRW5ITVJ?
QIMR-WIL NYWz[2dGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoH4TWM2OD1zN{muOlQ3KM7:TR?= MYrTRW5ITVJ?
NCI-H1395 NFzBU4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInsVpJKSzVyPUG3PU46QTZizszN MWnTRW5ITVJ?
NOMO-1 NGjNdZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17Tc2lEPTB;MUiyMlg2KM7:TR?= NWrn[ZdmW0GQR1XS
GI-ME-N MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTF6Nz65Olkh|ryP NFS4bnNUSU6JRWK=
KMS-12-PE NXXzO|U5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkX0TWM2OD1zOEmuNlc{KM7:TR?= MWnTRW5ITVJ?
Daudi NVzyOVBsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Xi[WlEPTB;MUmxMlEzQCEQvF2= MlPXV2FPT0WU
LB996-RCC MoLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rlSmlEPTB;MUmxMlY6QSEQvF2= MnvVV2FPT0WU
NCI-H2107 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTF7Mz63N|kh|ryP M3HScXNCVkeHUh?=
SK-PN-DW NGnoR3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDiSnJKSzVyPUG5OE44OTlizszN MWjTRW5ITVJ?
MC-CAR MmL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnSS3piUUN3ME2yNFIvOjV|IN88US=> M1fo[XNCVkeHUh?=
SNB75 NIq5R4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn36TWM2OD1{MkGuPVQh|ryP NET1WFRUSU6JRWK=
ES4 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTJ{Mz63PFMh|ryP MVPTRW5ITVJ?
KARPAS-422 NEPyT3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DMe2lEPTB;MkK4MlM2OiEQvF2= MoCxV2FPT0WU
NCI-H1648 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTJ{OT60PFkh|ryP MWfTRW5ITVJ?
ES6 MkPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXxTWM2OD1{M{muOFMh|ryP NVzjflNxW0GQR1XS
KNS-81-FD NWDJXo1{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU[1UmZDUUN3ME2yOFEvOTl5IN88US=> MWLTRW5ITVJ?
JAR MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTJ3Nj6yNlUh|ryP M2H0UXNCVkeHUh?=
NB1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTJ4MD61NVYh|ryP MWfTRW5ITVJ?
D-336MG M3TMXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkO5TWM2OD1{NkCuOlk5KM7:TR?= MlHKV2FPT0WU
BC-3 NXT0[4VyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjlbHpKSzVyPUK2OU4yPzhizszN NXnpdZVyW0GQR1XS
HCC2218 NVXn[21rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTJ4Nj60NVUh|ryP M1POXXNCVkeHUh?=
TE-9 MoLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvtdZlqUUN3ME2yOlYvPjJ5IN88US=> NFK0WVRUSU6JRWK=
LB1047-RCC NX\3dnBZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfj[pNtUUN3ME2yOlYvPzV|IN88US=> MXXTRW5ITVJ?
CTB-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;aOYdKSzVyPUK2PU46PzNizszN NVqzNGhLW0GQR1XS
NB7 MoDMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fRfmlEPTB;MkexJO69VQ>? NVfS[JNjW0GQR1XS
ST486 NVXadY1lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLjeIpKSzVyPUK3O{41OTJizszN NH\HVXVUSU6JRWK=
HCC1187 MoPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LmfmlEPTB;MkiyMlgyOSEQvF2= NILhR3lUSU6JRWK=
NCI-SNU-16 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXqR3lKSzVyPUK4OE4zPDhizszN Ml25V2FPT0WU
COR-L279 Ml;ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPuSYhKSzVyPUK5NU42QDRizszN MXfTRW5ITVJ?
ES8 NF\seopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlf4TWM2OD1{OUSuNVgzKM7:TR?= M3\XdHNCVkeHUh?=
U-698-M NHz1fldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELQSVVKSzVyPUK5PE4zPDNizszN MVrTRW5ITVJ?
HEL NGjTNFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml21TWM2OD1|MEmuNVQ6KM7:TR?= MnfqV2FPT0WU
KINGS-1 MnPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\yZmp{UUN3ME2zNVAvPjd2IN88US=> M{TPVnNCVkeHUh?=
KY821 NVThdVkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTrTWM2OD1|M{[uOVk2KM7:TR?= M4PFW3NCVkeHUh?=
MZ1-PC NFTlRWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzGV|ZKSzVyPUO0OU43OThizszN MorKV2FPT0WU
LS-411N MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3z3OGlEPTB;M{W0MlY3KM7:TR?= MYXTRW5ITVJ?
SIG-M5 NU\aSnp5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHOW4xwUUN3ME2zOVkvPzh{IN88US=> NYDmPI9nW0GQR1XS
HT NWfQSIpWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvqTWM2OD1|NkeuO|EyKM7:TR?= Moj0V2FPT0WU
HC-1 NH7afFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmSyTWM2OD1|NkeuO|g4KM7:TR?= MXfTRW5ITVJ?
NCI-H1694 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnv1TWM2OD1|N{KuPVM1KM7:TR?= NF\hbXhUSU6JRWK=
BB65-RCC NYq0dWFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fHRWlEPTB;M{e2MlI1PSEQvF2= MVjTRW5ITVJ?
HAL-01 MnztS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWP1OZdwUUN3ME2zO|kvQDN6IN88US=> NES4T2xUSU6JRWK=
ARH-77 NFyyTplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE[5eYRKSzVyPUO5OE4xODhizszN NH\4c3ZUSU6JRWK=
MZ7-mel NEi3fotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTFTWM2OD1|OUeuNlM{KM7:TR?= MoHlV2FPT0WU
SIMA M{j0emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rMeWlEPTB;NECzMlk{OyEQvF2= M1LZ[3NCVkeHUh?=
DG-75 MkXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkP0TWM2OD12MUWuOlk5KM7:TR?= NFzDeW1USU6JRWK=
HUTU-80 NVS1cWN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnWXlhKSzVyPUSxPU4yQDVizszN NVjicZVOW0GQR1XS
KNS-42 NFHaPVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTR{NT64NVUh|ryP NFfhWZlUSU6JRWK=
SH-4 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTR{Nz61OlUh|ryP NWXofYgxW0GQR1XS
L-540 MorqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLrenVKSzVyPUSzNU4xOzFizszN NWjzUYVsW0GQR1XS
NB10 NWfsRo0xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\XV3FJUUN3ME20OFEvOjN2IN88US=> NVjqWYRvW0GQR1XS
ES1 NWPsbW9XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTX[JRmUUN3ME20OVIvPzV|IN88US=> NF[3N4JUSU6JRWK=
KMOE-2 NGjGNo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\ZU2RmUUN3ME20OVYvPzFzIN88US=> MVXTRW5ITVJ?
MC116 NI\jem9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTR3OD6xNVYh|ryP NE\PfpdUSU6JRWK=
RCC10RGB NHnMdZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPqTYNKSzVyPUS2NE4xODVizszN MoHYV2FPT0WU
RL95-2 NILwNJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2qxfGlEPTB;NE[wMlI{PyEQvF2= MU\TRW5ITVJ?
Raji M2fST2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;oTWM2OD12NkiuNVQ{KM7:TR?= MUfTRW5ITVJ?
CAS-1 Ml7US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrifZM3UUN3ME20O|IvODd|IN88US=> M{TicXNCVkeHUh?=
Calu-6 M321[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnGdnNKSzVyPUS3OU4zPjVizszN NFHsZYlUSU6JRWK=
KG-1 MmPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTR5OD60OEDPxE1? Ml\lV2FPT0WU
LB771-HNC M{[zTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;lbmdKSzVyPUS4Nk4zOzJizszN NF\ueGRUSU6JRWK=
ACN Mk[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLmTWM2OD12OUOuOVk6KM7:TR?= NUjER5pHW0GQR1XS
KM12 NWrDSpFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTFTZhuUUN3ME20PVYvPTh7IN88US=> MVPTRW5ITVJ?

... 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 2年-20℃
6月-80℃in solvent
別名 11-deoxojervine
溶解度 (25°C) * In vitro DMF 10 mg/mL warmed (24.29 mM)
エタノール 2 mg/mL warmed (4.85 mM)
<1 mg/mL (<1 mM)
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)-

カスタマーフィードバック (4)


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Source Cancer Lett, 2012, 322, 169-176. Cyclopamine purchased from Selleck
Method Western blotting, real-time RT-PCR
Cell Lines pancreatic cancer cell
Concentrations 10 μM
Incubation Time 48 h
Results Cyclopamine significantly decreased pancreatic cancer invasion (Fig. A), reversed the down-regulation of E-cadherin and up-regulation of vimentin (Fig. B and C), and reduced the expression of Gli-1 even in the presence of SDF-1 (Fig. B).

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Source Cancer Res, 2012, 72, 2262-74. Cyclopamine purchased from Selleck
Method [3H]thymidine incorporation assay, Western blot
Cell Lines melanoma cells, A-375 cells
Concentrations 5-10 μmol/L
Incubation Time 48 h
Results Our results show that low concentrations of cyclopamine (5-10 μmol/L) were effective in blocking the proproliferative effects of Cav1KO-CM on B16F10 melanoma cells. Interestingly, the proliferation of B16F10 cells incubated with WT-CM containing cyclopamine remains unchanged (Fig. A). Similarly, cyclopamine prevented the proproliferative effects of conditioned medium from serum-activated hTBJ1-shCAV1 cells on A-375 human melanoma cells (Fig. B)

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Rating
Source Exp Hematol, 2012, 40, 418-27. Cyclopamine purchased from Selleck
Method MTT assay
Cell Lines CD34+ cells, CD34- cells
Concentrations 10 μM
Incubation Time 24/72 h
Results 10 μM cyclopamine was administered to CD34+ and CD34- cells. After 72 hours cultivation, total cell number was about 0.73-fold of control in CD34+ cells group (p < 0.001), and it was about 0.92-fold of control (p = 0.038) in CD34- cells group (Fig. A). Cyclopamine induced apoptosis of CD34+ progenitor cells and CD34- leukemia cells; however, CD34+ cells were more sensitive to cyclopamine than CD34- cells (p < 0.001). Cyclopamine also induced apoptosis of K562 cells in a time-dependent manner, as measured by MTT assay. This effect could not be salvaged by exogenous Shh peptide, confirming the fact that SMO locates downstream of SHH in Shh signaling (Fig. B)

Click to enlarge
Rating
Source Dr. Yong-Weon Yi from Georgetown University Medical Center. Cyclopamine purchased from Selleck
Method MTT assays
Cell Lines UWB1.289 cells
Concentrations 0.01-100 μM
Incubation Time 72 h
Results Cyclopamine potently inhibited the survival of UWB1.289 cells.

文献中の引用 (14)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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