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 NIHNfGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTVwOE[2OkDPxE1? NVq0T5FYW0GQR1XS
DOHH-2 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nISGlEPTB;OT6zOVY5QSEQvF2= MkO1V2FPT0WU
no-10 M3j2O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTlwOUCzPUDPxE1? NGe0TW9USU6JRWK=
LS-513 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnKOm1JUUN3ME2xNU4{PTR5IN88US=> MnXxV2FPT0WU
ALL-PO NX;1dJZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILDbFVKSzVyPUGxMlc4OzRizszN M4\Dc3NCVkeHUh?=
8-MG-BA NHTrcFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfRV5NKSzVyPUGzMlEyOjNizszN NUmxW5ozW0GQR1XS
RPMI-8402 NUiyTFJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPZbVFKSzVyPUG1Mlg2OzdizszN NIfacoVUSU6JRWK=
EoL-1-cell NF7tR3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTiTWM2OD1zOD61PVQ5KM7:TR?= NVu3[lg4W0GQR1XS
NALM-6 Ml;SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3z3TGlEPTB;MUmuNFE3PyEQvF2= NVXid|dVW0GQR1XS
DEL M2HLe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLRTWM2OD1{MD6xOFcyKM7:TR?= MkfHV2FPT0WU
SR M4nXTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrYT3pKSzVyPUKzMlY4OTVizszN Mm\jV2FPT0WU
697 NUjLbpJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETCWmpKSzVyPUK2MlYyPTVizszN M2nSW3NCVkeHUh?=
COLO-829 NEHyUoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTJ4Lki0PFMh|ryP M{\SNXNCVkeHUh?=
EVSA-T Ml;qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTJ5LkW1OlEh|ryP NH\Gc2VUSU6JRWK=
ATN-1 MmDDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPkTWM2OD1|MT6yN|I6KM7:TR?= MV;TRW5ITVJ?
L-363 NUjRfo5GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTNzLke0OlEh|ryP M3W2WHNCVkeHUh?=
LAMA-84 M13tT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHnTWM2OD1|Mj61NlEyKM7:TR?= MnHYV2FPT0WU
NOS-1 M{HIbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\lfphKSzVyPUO0MlI6PTZizszN MWHTRW5ITVJ?
BB30-HNC NGj4fYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoS4TWM2OD1|ND6zN|A3KM7:TR?= M3\mSHNCVkeHUh?=
BC-1 NET2WZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\OelZKSzVyPUO3Mlk4PDZizszN NUn5bVk1W0GQR1XS
IST-SL2 NYHMcmt7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\FTWM2OD1|OD6yNlQh|ryP M1nkVXNCVkeHUh?=
D-392MG Ml7OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnP3TWM2OD12MD6yNlE2KM7:TR?= Ml63V2FPT0WU
no-11 NGnXXpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4S0UGlEPTB;NECuOVUzOSEQvF2= NFnMVnFUSU6JRWK=
LC4-1 MkXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYO1dIllUUN3ME20NE45PzF4IN88US=> MnvOV2FPT0WU
A388 Mk\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfUTWM2OD12Mj61PFQ5KM7:TR?= MoTXV2FPT0WU
NTERA-S-cl-D1 MmX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17uSmlEPTB;NEKuO|A4PCEQvF2= MX;TRW5ITVJ?
CESS NHSwV5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmniTWM2OD12ND6yNlMzKM7:TR?= MnXkV2FPT0WU
RS4-11 M1jIeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIr2UI9KSzVyPUS5MlA6OzhizszN NV\Ib3lOW0GQR1XS
MS-1 M4jDbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjpTWM2OD13MD65N|UyKM7:TR?= NXn2UHJkW0GQR1XS
CTV-1 NVryUHNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPlPJRiUUN3ME21NU4xPzRizszN M4Kwd3NCVkeHUh?=
D-502MG MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTVzLk[yO|Eh|ryP MojTV2FPT0WU
ML-2 NFzTWIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTV{LkmxPVUh|ryP MmS1V2FPT0WU
SK-NEP-1 M3P6S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoG2TWM2OD13Mz6zPVI{KM7:TR?= NWrlU|NpW0GQR1XS
LOXIMVI M1;QNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTV|LkW4PFQh|ryP NWnpPIFyW0GQR1XS
DJM-1 NV:1eHp6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULKRpJOUUN3ME21Ok4{OzlzIN88US=> MUTTRW5ITVJ?
GI-1 NF35S2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUns[mNRUUN3ME21Ok43OTR7IN88US=> NXy1c5dvW0GQR1XS
IST-MES1 NX7LWG0zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjMbmtKSzVyPU[wMlU1QTNizszN NHPhe2FUSU6JRWK=
MV-4-11 NVTLXZI2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTTUmo4UUN3ME22NE43PTN6IN88US=> NGPXb2lUSU6JRWK=
OVCAR-4 MoLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\r[GlEPTB;NkOuOVY2PyEQvF2= NV7EUVlrW0GQR1XS
KE-37 Mn65S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXBWGI1UUN3ME22Ok4zPjZ6IN88US=> MX7TRW5ITVJ?
D-542MG MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;HNJBKSzVyPU[4MlQyOzVizszN NH\zelVUSU6JRWK=
MHH-PREB-1 NIr3U5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fyXWlEPTB;N{KuPFQ1OSEQvF2= MVPTRW5ITVJ?
MRK-nu-1 NEPTTW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrINYZKSzVyPUezMlQ4ODVizszN M4K2OnNCVkeHUh?=
D-247MG M3vje2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPxZVJKSzVyPUezMlU1PDJizszN MnzoV2FPT0WU
OCI-AML2 NInlPZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TMSWlEPTB;N{[uPVM3QSEQvF2= MWDTRW5ITVJ?
LP-1 M3nlbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTh{Lki3N|Eh|ryP NUjVVoh7W0GQR1XS
HCC1599 M2XINWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jSemlEPTB;OESuNlg{PyEQvF2= M4m5b3NCVkeHUh?=
KARPAS-45 NW[wRWM{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvDTWM2OD16ND62PVkzKM7:TR?= M1niSHNCVkeHUh?=
BE-13 NUG5OHFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHUTJJNUUN3ME25PU4xPDd5IN88US=> NESzdZdUSU6JRWK=
GCIY MoryS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTl7LkC5OVQh|ryP NHvtdZRUSU6JRWK=
BV-173 NYTuTIdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjnNoRRUUN3ME2xNFAvOzJ3IN88US=> NVvsc3RxW0GQR1XS
LB2518-MEL NX\kXlY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTtOm9KSzVyPUGwNE44QDlizszN NVfT[|FRW0GQR1XS
KS-1 NH\MNnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkewTWM2OD1zMEGuOlM6KM7:TR?= NF31UG9USU6JRWK=
MOLT-16 M3;iUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTFyND65PFYh|ryP M3rWdnNCVkeHUh?=
NCI-H1770 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PJTmlEPTB;MUC4Mlc5PCEQvF2= NHLWWYlUSU6JRWK=
NCI-H82 NXLtO|RNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TqRmlEPTB;MUGwMlk4PiEQvF2= MkHJV2FPT0WU
NCCIT MlXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jNNmlEPTB;MUGyMlUzQSEQvF2= Mo\QV2FPT0WU
KALS-1 Mkf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWS2UpE4UUN3ME2xNVUvQTRzIN88US=> NYTaNnB7W0GQR1XS
LB2241-RCC MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTFzNj62O|kh|ryP Ml7YV2FPT0WU
HH NWD4[W9ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfRbGdKSzVyPUGxO{4{QTVizszN MWLTRW5ITVJ?
HD-MY-Z MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnTfWVKSzVyPUGxPE41QDhizszN MVHTRW5ITVJ?
EB-3 M2S4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TGbmlEPTB;MUKzMlA6PCEQvF2= NFTndYdUSU6JRWK=
BL-70 NWHrNpp1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{n6XmlEPTB;MUKzMlEzPyEQvF2= NYWzdmkzW0GQR1XS
K-562 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTF{Nj6yOFUh|ryP M{TabnNCVkeHUh?=
HT-144 M1L3[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTF|Mz6xOlQh|ryP NULrV2lvW0GQR1XS
PF-382 MnTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojnTWM2OD1zM{SuN|YyKM7:TR?= MkXVV2FPT0WU
RPMI-8226 NV6wRXd5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIC4fmdKSzVyPUGzOU4xPDVizszN NFT2RlFUSU6JRWK=
NCI-H1355 M3LVWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvBN4NKSzVyPUGzOU42QDdizszN NWL5d3FpW0GQR1XS
LXF-289 NI\uZZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;YOWlEPTB;MUO5Mlc5OSEQvF2= NInE[2FUSU6JRWK=
NCI-H69 M4ruNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\ZXIJKSzVyPUG0Nk46OzJizszN NGnmSnRUSU6JRWK=
SK-MEL-1 NYTZV5VpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTF2Nz6xN{DPxE1? NUXacmpJW0GQR1XS
KARPAS-299 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDuTWM2OD1zNEmuNVIh|ryP M4ru[nNCVkeHUh?=
GB-1 M{T4NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Pl[mlEPTB;MUS5MlMzOiEQvF2= M3XkXXNCVkeHUh?=
CMK NYnGeGdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTF2OT61NVUh|ryP NGm0PZBUSU6JRWK=
MPP-89 MoPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH22OXVKSzVyPUG1Ok4xOzVizszN MmP6V2FPT0WU
KU812 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTITWM2OD1zNkGuPVAzKM7:TR?= MXXTRW5ITVJ?
REH NIPZfHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjaTWM2OD1zNkKuNVI2KM7:TR?= M{HINHNCVkeHUh?=
NEC8 NUjwOWE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjReGxSUUN3ME2xOlUvODJ4IN88US=> MofyV2FPT0WU
KP-N-YS Mni2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3PXVFKSzVyPUG2PE4{QTVizszN MXzTRW5ITVJ?
Ramos-2G6-4C10 NWflVFF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIf3S5JKSzVyPUG2PU46OTVizszN Mn\6V2FPT0WU
Becker MofqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnj4TWM2OD1zN{SuNVgh|ryP NHjTfnJUSU6JRWK=
LB647-SCLC NHjMNWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7yTWM2OD1zN{WuPFQ2KM7:TR?= MmjuV2FPT0WU
LU-139 NYPLN2dDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTF5OD6wNVkh|ryP MnW0V2FPT0WU
QIMR-WIL NH3mb4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEj4[GtKSzVyPUG3PU43PDZizszN NVy4fXpbW0GQR1XS
NCI-H1395 MnfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;NNZBKSzVyPUG3PU46QTZizszN NHXVU|dUSU6JRWK=
NOMO-1 M{H5SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlu2TWM2OD1zOEKuPFUh|ryP MU\TRW5ITVJ?
GI-ME-N NHOxSmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLETWM2OD1zOEeuPVY6KM7:TR?= MVPTRW5ITVJ?
KMS-12-PE M2nnWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTMTIxKSzVyPUG4PU4zPzNizszN MnOxV2FPT0WU
Daudi NFrrWGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4qxT2lEPTB;MUmxMlEzQCEQvF2= MnjtV2FPT0WU
LB996-RCC MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPXbIhKSzVyPUG5NU43QTlizszN M1iwN3NCVkeHUh?=
NCI-H2107 NUn5V2JpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jET2lEPTB;MUmzMlc{QSEQvF2= NGXyTVBUSU6JRWK=
SK-PN-DW MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTF7ND63NVkh|ryP MYfTRW5ITVJ?
MC-CAR MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzRUm54UUN3ME2yNFIvOjV|IN88US=> NGf2b45USU6JRWK=
SNB75 M4nNXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3f6ZmlEPTB;MkKxMlk1KM7:TR?= NEP0e2xUSU6JRWK=
ES4 NVO5TG0zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLkTWM2OD1{MkOuO|g{KM7:TR?= NFT4ZotUSU6JRWK=
KARPAS-422 M2nzcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3FTWM2OD1{MkiuN|UzKM7:TR?= Mlu5V2FPT0WU
NCI-H1648 NGnC[lRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4P2cmlEPTB;MkK5MlQ5QSEQvF2= M3rBb3NCVkeHUh?=
ES6 NXXLUVVwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoK1TWM2OD1{M{muOFMh|ryP NEP1TmdUSU6JRWK=
KNS-81-FD MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrPcnhKSzVyPUK0NU4yQTdizszN MljPV2FPT0WU
JAR NUjQfG4yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\oTWM2OD1{NU[uNlI2KM7:TR?= Ml7NV2FPT0WU
NB1 MorwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTJ4MD61NVYh|ryP M1HNVHNCVkeHUh?=
D-336MG NGC2ZoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYX0NJp7UUN3ME2yOlAvPjl6IN88US=> MlfoV2FPT0WU
BC-3 NGTVS5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTJ4NT6xO|gh|ryP NYLGeIg1W0GQR1XS
HCC2218 NFOwT3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEX2ZZZKSzVyPUK2Ok41OTVizszN NI\LO4xUSU6JRWK=
TE-9 MnHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn:yTWM2OD1{Nk[uOlI4KM7:TR?= NXPFN2Z3W0GQR1XS
LB1047-RCC M1vYOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPZTWM2OD1{Nk[uO|U{KM7:TR?= NIO2[HNUSU6JRWK=
CTB-1 MnXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTRTWM2OD1{NkmuPVc{KM7:TR?= MmrFV2FPT0WU
NB7 NFS4dIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rodGlEPTB;MkexJO69VQ>? NHnQdFBUSU6JRWK=
ST486 NELjNGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYq2SYQ{UUN3ME2yO|cvPDF{IN88US=> MlO4V2FPT0WU
HCC1187 NGXVXpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4ruOmlEPTB;MkiyMlgyOSEQvF2= Ml7SV2FPT0WU
NCI-SNU-16 Mm\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXTZnBKSzVyPUK4OE4zPDhizszN M{m3VHNCVkeHUh?=
COR-L279 MoT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjud|V6UUN3ME2yPVEvPTh2IN88US=> MWnTRW5ITVJ?
ES8 M4DBeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTISJhKSzVyPUK5OE4yQDJizszN NGS5S4ZUSU6JRWK=
U-698-M MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHz2NopKSzVyPUK5PE4zPDNizszN MUHTRW5ITVJ?
HEL NEDTRXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTNyOT6xOFkh|ryP MUDTRW5ITVJ?
KINGS-1 NEXaPFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrFb3lKSzVyPUOxNE43PzRizszN NUHLdGJrW0GQR1XS
KY821 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfTeWFKSzVyPUOzOk42QTVizszN NVn6OGc1W0GQR1XS
MZ1-PC MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3:4emlEPTB;M{S1MlYyQCEQvF2= M4jEVXNCVkeHUh?=
LS-411N NFzVTo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTwTWM2OD1|NUSuOlYh|ryP MmnxV2FPT0WU
SIG-M5 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2i0N2lEPTB;M{W5Mlc5OiEQvF2= M1zrTHNCVkeHUh?=
HT MofaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTDTWM2OD1|NkeuO|EyKM7:TR?= NWTPOXB7W0GQR1XS
HC-1 NV3LZYF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{C5d2lEPTB;M{[3Mlc5PyEQvF2= NESxXlRUSU6JRWK=
NCI-H1694 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\ITWM2OD1|N{KuPVM1KM7:TR?= MUfTRW5ITVJ?
BB65-RCC Mn[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\mTWlEPTB;M{e2MlI1PSEQvF2= NFuzW4RUSU6JRWK=
HAL-01 M4fhZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTkS2RKSzVyPUO3PU45OzhizszN MY\TRW5ITVJ?
ARH-77 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HmWmlEPTB;M{m0MlAxQCEQvF2= MlOxV2FPT0WU
MZ7-mel NHvjT2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTN7Nz6yN|Mh|ryP MnnEV2FPT0WU
SIMA Mlr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjwfpp7UUN3ME20NFMvQTN|IN88US=> MWfTRW5ITVJ?
DG-75 NX7ldZFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTFTFdYUUN3ME20NVUvPjl6IN88US=> MWnTRW5ITVJ?
HUTU-80 MnWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTqb25KSzVyPUSxPU4yQDVizszN NYPuO5NvW0GQR1XS
KNS-42 MmLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTR{NT64NVUh|ryP M3jiN3NCVkeHUh?=
SH-4 MnPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTR{Nz61OlUh|ryP MUjTRW5ITVJ?
L-540 M3TUfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTR|MT6wN|Eh|ryP MYrTRW5ITVJ?
NB10 M3jFSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnp[WRuUUN3ME20OFEvOjN2IN88US=> NIL5eFZUSU6JRWK=
ES1 NGXTV4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTR3Mj63OVMh|ryP M{DPO3NCVkeHUh?=
KMOE-2 NF6wZ4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPUPIpKSzVyPUS1Ok44OTFizszN MnLEV2FPT0WU
MC116 NITpeoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPwXIhKSzVyPUS1PE4yOTZizszN MlrBV2FPT0WU
RCC10RGB M17rdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvITWM2OD12NkCuNFA2KM7:TR?= MUHTRW5ITVJ?
RL95-2 MnLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\GPWlEPTB;NE[wMlI{PyEQvF2= NWTiU|hTW0GQR1XS
Raji NH;HNpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3vW3FKSzVyPUS2PE4yPDNizszN NYq5fHV5W0GQR1XS
CAS-1 MoG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\qTJd3UUN3ME20O|IvODd|IN88US=> NHjaNGVUSU6JRWK=
Calu-6 NHjWOGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rQfWlEPTB;NEe1MlI3PSEQvF2= MlvvV2FPT0WU
KG-1 NXnzc49ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;0SmpTUUN3ME20O|gvPDRizszN M1jCRnNCVkeHUh?=
LB771-HNC MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rHU2lEPTB;NEiyMlI{OiEQvF2= MWDTRW5ITVJ?
ACN MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jadGlEPTB;NEmzMlU6QSEQvF2= MV;TRW5ITVJ?
KM12 M4npcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTR7Nj61PFkh|ryP MnrXV2FPT0WU

... 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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