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 NXLBUolwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGi4VFJKSzVyPUWuPFY3PiEQvF2= MYTTRW5ITVJ?
DOHH-2 M3ezWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TWPGlEPTB;OT6zOVY5QSEQvF2= NYHEWHBwW0GQR1XS
no-10 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnGOlJzUUN3ME25MlkxOzlizszN NWLzS3FyW0GQR1XS
LS-513 NXW2VIY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTFzLkO1OFch|ryP NIjYTJFUSU6JRWK=
ALL-PO NETVRoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfwVXE2UUN3ME2xNU44PzN2IN88US=> M1TGXnNCVkeHUh?=
8-MG-BA MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmG1TWM2OD1zMz6xNVI{KM7:TR?= NI\1e4ZUSU6JRWK=
RPMI-8402 M{\Cemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXSXXIxUUN3ME2xOU45PTN5IN88US=> MoL6V2FPT0WU
EoL-1-cell MkfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTF6LkW5OFgh|ryP M1zpZXNCVkeHUh?=
NALM-6 M1HMUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3e5XmlEPTB;MUmuNFE3PyEQvF2= M2DHTHNCVkeHUh?=
DEL NXq0WmRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\DeWlEPTB;MkCuNVQ4OSEQvF2= MWLTRW5ITVJ?
SR Mor2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonwTWM2OD1{Mz62O|E2KM7:TR?= NH;wZWJUSU6JRWK=
697 M4GzXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonFTWM2OD1{Nj62NVU2KM7:TR?= NUnSUmgyW0GQR1XS
COLO-829 Ml\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDPb4RKSzVyPUK2Mlg1QDNizszN M3;yc3NCVkeHUh?=
EVSA-T NWHpNJY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIL3fXdKSzVyPUK3MlU2PjFizszN NFvDV5FUSU6JRWK=
ATN-1 NWTEVWluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjyUnVqUUN3ME2zNU4zOzJ7IN88US=> MVrTRW5ITVJ?
L-363 NUT0TlBtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGryZY9KSzVyPUOxMlc1PjFizszN NXLYSHNHW0GQR1XS
LAMA-84 MlTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTN{LkWyNVEh|ryP MUDTRW5ITVJ?
NOS-1 MoDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnPellLUUN3ME2zOE4zQTV4IN88US=> MXPTRW5ITVJ?
BB30-HNC Mn;SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTvTWM2OD1|ND6zN|A3KM7:TR?= NV\tXVNFW0GQR1XS
BC-1 NFr3OYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;IUmlEPTB;M{euPVc1PiEQvF2= MXPTRW5ITVJ?
IST-SL2 Ml;YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYf1NnpVUUN3ME2zPE4zOjRizszN NVPhboFxW0GQR1XS
D-392MG Mn7lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LufGlEPTB;NECuNlIyPSEQvF2= MnjKV2FPT0WU
no-11 NHL5ZllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPMTWM2OD12MD61OVIyKM7:TR?= Mm\kV2FPT0WU
LC4-1 NVjRO|dWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETHXFZKSzVyPUSwMlg4OTZizszN MkLOV2FPT0WU
A388 NGPFemtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVKzV2tCUUN3ME20Nk42QDR6IN88US=> NHm0R5BUSU6JRWK=
NTERA-S-cl-D1 MmTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTR{LkewO|Qh|ryP MorNV2FPT0WU
CESS MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DqPGlEPTB;NESuNlI{OiEQvF2= NHPkeZVUSU6JRWK=
RS4-11 NWLYb2VxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYD1SHhvUUN3ME20PU4xQTN6IN88US=> MXHTRW5ITVJ?
MS-1 Mo[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7SNZF2UUN3ME21NE46OzVzIN88US=> MlHiV2FPT0WU
CTV-1 MoXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;lTWM2OD13MT6wO|Qh|ryP NXzMd49wW0GQR1XS
D-502MG NWH6dZBYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTVzLk[yO|Eh|ryP MWTTRW5ITVJ?
ML-2 NF\qcpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXBb2lKSzVyPUWyMlkyQTVizszN NHfPNphUSU6JRWK=
SK-NEP-1 NYjrS29LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37PVWlEPTB;NUOuN|kzOyEQvF2= M4ewVnNCVkeHUh?=
LOXIMVI MnjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fYXmlEPTB;NUOuOVg5PCEQvF2= NFSzVoZUSU6JRWK=
DJM-1 Mnj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTV4LkOzPVEh|ryP MXfTRW5ITVJ?
GI-1 M1;Ubmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XLVWlEPTB;NU[uOlE1QSEQvF2= NX\hWG9OW0GQR1XS
IST-MES1 MlPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnrTWM2OD14MD61OFk{KM7:TR?= Mn:2V2FPT0WU
MV-4-11 MnrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rqRmlEPTB;NkCuOlU{QCEQvF2= Ml3FV2FPT0WU
OVCAR-4 MlXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXJTWM2OD14Mz61OlU4KM7:TR?= M4\CRnNCVkeHUh?=
KE-37 MkfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUOxZ|BMUUN3ME22Ok4zPjZ6IN88US=> NInVco1USU6JRWK=
D-542MG M{jxPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTZ6LkSxN|Uh|ryP M1e1RXNCVkeHUh?=
MHH-PREB-1 NH;Wc|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nq[GlEPTB;N{KuPFQ1OSEQvF2= NGjx[pZUSU6JRWK=
MRK-nu-1 MkfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTd|LkS3NFUh|ryP MXHTRW5ITVJ?
D-247MG NF\YOGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjuVJFKSzVyPUezMlU1PDJizszN MWLTRW5ITVJ?
OCI-AML2 NIDzSYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYO0XlBjUUN3ME23Ok46OzZ7IN88US=> Mof1V2FPT0WU
LP-1 NEjvSVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXH0c2VFUUN3ME24Nk45PzNzIN88US=> M{nIdHNCVkeHUh?=
HCC1599 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnSUoZGUUN3ME24OE4zQDN5IN88US=> MV3TRW5ITVJ?
KARPAS-45 NF;iUFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TTSWlEPTB;OESuOlk6OiEQvF2= MVPTRW5ITVJ?
BE-13 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjjOFVKSzVyPUm5MlA1PzdizszN MV\TRW5ITVJ?
GCIY MlrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\3[WlEPTB;OUmuNFk2PCEQvF2= M{HC[XNCVkeHUh?=
BV-173 NGjUTZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnKTWM2OD1zMECuN|I2KM7:TR?= M4jtNnNCVkeHUh?=
LB2518-MEL NHHvOIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGniWGxKSzVyPUGwNE44QDlizszN MV7TRW5ITVJ?
KS-1 M4iwZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUS2[|I2UUN3ME2xNFEvPjN7IN88US=> MYPTRW5ITVJ?
MOLT-16 MlnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTFyND65PFYh|ryP NV7BOJI{W0GQR1XS
NCI-H1770 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH65e3hKSzVyPUGwPE44QDRizszN NVvYOotkW0GQR1XS
NCI-H82 MlmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jSZWlEPTB;MUGwMlk4PiEQvF2= MWXTRW5ITVJ?
NCCIT M37IVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknCTWM2OD1zMUKuOVI6KM7:TR?= Mm\kV2FPT0WU
KALS-1 M2HZb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\YO5BKSzVyPUGxOU46PDFizszN MV7TRW5ITVJ?
LB2241-RCC MnywS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTFzNj62O|kh|ryP NVXnZm9IW0GQR1XS
HH M2\FUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mon6TWM2OD1zMUeuN|k2KM7:TR?= M3vxNXNCVkeHUh?=
HD-MY-Z MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTFzOD60PFgh|ryP MY\TRW5ITVJ?
EB-3 M1jPS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTF{Mz6wPVQh|ryP M2[wV3NCVkeHUh?=
BL-70 NF76NmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPkUnFpUUN3ME2xNlMvOTJ5IN88US=> NGrafpdUSU6JRWK=
K-562 NEXrfYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTF{Nj6yOFUh|ryP NYfld21LW0GQR1XS
HT-144 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHSy[4pKSzVyPUGzN{4yPjRizszN M4PQbHNCVkeHUh?=
PF-382 NIDTOpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXETWM2OD1zM{SuN|YyKM7:TR?= MX\TRW5ITVJ?
RPMI-8226 NEnFTWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTF|NT6wOFUh|ryP NGDMTnpUSU6JRWK=
NCI-H1355 NI\lSnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTF|NT61PFch|ryP Ml;jV2FPT0WU
LXF-289 MkX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTF|OT63PFEh|ryP NX[xTYF3W0GQR1XS
NCI-H69 Mnn6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEn6SlZKSzVyPUG0Nk46OzJizszN M1:wPXNCVkeHUh?=
SK-MEL-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHCXlFKSzVyPUG0O{4yOyEQvF2= M{TpXXNCVkeHUh?=
KARPAS-299 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjxU2pKSzVyPUG0PU4yOiEQvF2= M4DIRXNCVkeHUh?=
GB-1 Mn7sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rSSmlEPTB;MUS5MlMzOiEQvF2= M4rs[nNCVkeHUh?=
CMK NEn3W5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fYfmlEPTB;MUS5MlUyPSEQvF2= M4L5THNCVkeHUh?=
MPP-89 Mk\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFGwcXJKSzVyPUG1Ok4xOzVizszN NWXvZ2JvW0GQR1XS
KU812 MkPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TWWWlEPTB;MU[xMlkxOiEQvF2= MkC5V2FPT0WU
REH MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TjXGlEPTB;MU[yMlEzPSEQvF2= MXjTRW5ITVJ?
NEC8 M4LmVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TKbGlEPTB;MU[1MlAzPiEQvF2= NX\iZXE4W0GQR1XS
KP-N-YS M2j4XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\BS5N7UUN3ME2xOlgvOzl3IN88US=> MUDTRW5ITVJ?
Ramos-2G6-4C10 NE\oSnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTF4OT65NVUh|ryP NIfGfpVUSU6JRWK=
Becker MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPiV41KSzVyPUG3OE4yQCEQvF2= NX7mbnFYW0GQR1XS
LB647-SCLC M4rBN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvnTWM2OD1zN{WuPFQ2KM7:TR?= NIfrdG5USU6JRWK=
LU-139 M4jJ[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTF5OD6wNVkh|ryP M1;KfXNCVkeHUh?=
QIMR-WIL M2fodWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTOWnFIUUN3ME2xO|kvPjR4IN88US=> Mkf6V2FPT0WU
NCI-H1395 M{[2bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknMTWM2OD1zN{muPVk3KM7:TR?= MofJV2FPT0WU
NOMO-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;HVGlEPTB;MUiyMlg2KM7:TR?= NWXtcJV[W0GQR1XS
GI-ME-N MoH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7Xb4lKSzVyPUG4O{46PjlizszN MUDTRW5ITVJ?
KMS-12-PE MoXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\mTZdrUUN3ME2xPFkvOjd|IN88US=> NGTBNHdUSU6JRWK=
Daudi Ml3WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHMTWM2OD1zOUGuNVI5KM7:TR?= MnqxV2FPT0WU
LB996-RCC NWrWcoVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1ryeWlEPTB;MUmxMlY6QSEQvF2= MkiwV2FPT0WU
NCI-H2107 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrRTWM2OD1zOUOuO|M6KM7:TR?= NXnZTm1kW0GQR1XS
SK-PN-DW NYr2UVc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTF7ND63NVkh|ryP MnSxV2FPT0WU
MC-CAR NV7BRoNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHO3[HhKSzVyPUKwNk4zPTNizszN MkXhV2FPT0WU
SNB75 NYnBOFBHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jDbGlEPTB;MkKxMlk1KM7:TR?= NYrm[|VyW0GQR1XS
ES4 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXGwVW1QUUN3ME2yNlMvPzh|IN88US=> NYTsSJJ5W0GQR1XS
KARPAS-422 MnfGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXzTWM2OD1{MkiuN|UzKM7:TR?= MUXTRW5ITVJ?
NCI-H1648 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\tToZKSzVyPUKyPU41QDlizszN MVfTRW5ITVJ?
ES6 M3WzWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjmTWM2OD1{M{muOFMh|ryP MnzXV2FPT0WU
KNS-81-FD M{OyNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\Ke3BKSzVyPUK0NU4yQTdizszN NGO0bHZUSU6JRWK=
JAR NVXqVHNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTJ3Nj6yNlUh|ryP MmLJV2FPT0WU
NB1 MmrMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTJ4MD61NVYh|ryP M1i4cXNCVkeHUh?=
D-336MG MmLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoL4TWM2OD1{NkCuOlk5KM7:TR?= MW\TRW5ITVJ?
BC-3 NFSzN2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLYTWM2OD1{NkWuNVc5KM7:TR?= MWfTRW5ITVJ?
HCC2218 M1v0fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTJ4Nj60NVUh|ryP NUXpV3NoW0GQR1XS
TE-9 M{[0SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHRZZNKSzVyPUK2Ok43OjdizszN NFLwTmdUSU6JRWK=
LB1047-RCC M{XkUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWW3TYNsUUN3ME2yOlYvPzV|IN88US=> Mm\PV2FPT0WU
CTB-1 MlTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPkfINKSzVyPUK2PU46PzNizszN NH63[VlUSU6JRWK=
NB7 M4j3UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTJ5MTFOwG0> MmW1V2FPT0WU
ST486 MoPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmT0TWM2OD1{N{euOFEzKM7:TR?= MYPTRW5ITVJ?
HCC1187 M{jUbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnq3TWM2OD1{OEKuPFEyKM7:TR?= MWTTRW5ITVJ?
NCI-SNU-16 NXTQTHFoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTJ6ND6yOFgh|ryP NWXo[FVPW0GQR1XS
COR-L279 M4DIZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PsbGlEPTB;MkmxMlU5PCEQvF2= M33U[3NCVkeHUh?=
ES8 M3KwU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;xPGlEPTB;Mkm0MlE5OiEQvF2= M3uyNXNCVkeHUh?=
U-698-M NHPGOYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUG2OWczUUN3ME2yPVgvOjR|IN88US=> NHzFfJNUSU6JRWK=
HEL MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4myfGlEPTB;M{C5MlE1QSEQvF2= NWXZbIg3W0GQR1XS
KINGS-1 Mnu2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHu1e5FKSzVyPUOxNE43PzRizszN NFHuO4hUSU6JRWK=
KY821 NIX4TFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUi0N5NKUUN3ME2zN|YvPTl3IN88US=> MnfqV2FPT0WU
MZ1-PC MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7y[|YyUUN3ME2zOFUvPjF6IN88US=> MUnTRW5ITVJ?
LS-411N NVviV2puT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlixTWM2OD1|NUSuOlYh|ryP MoXWV2FPT0WU
SIG-M5 M3fSZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTC[npJUUN3ME2zOVkvPzh{IN88US=> NHHSXoRUSU6JRWK=
HT MnG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkOwTWM2OD1|NkeuO|EyKM7:TR?= NH7qZoZUSU6JRWK=
HC-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrFTWM2OD1|NkeuO|g4KM7:TR?= M3;xdHNCVkeHUh?=
NCI-H1694 NEjNR4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvTNYZKSzVyPUO3Nk46OzRizszN Ml35V2FPT0WU
BB65-RCC Ml\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTN5Nj6yOFUh|ryP Mm\pV2FPT0WU
HAL-01 NH3SRnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIGySG1KSzVyPUO3PU45OzhizszN M2TzO3NCVkeHUh?=
ARH-77 M1rPcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1OxR2lEPTB;M{m0MlAxQCEQvF2= M4HD[HNCVkeHUh?=
MZ7-mel NEnoOY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF62V4RKSzVyPUO5O{4zOzNizszN MWDTRW5ITVJ?
SIMA M4LpVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4WxR2lEPTB;NECzMlk{OyEQvF2= NWLaeHZlW0GQR1XS
DG-75 NEDiSJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3xTWM2OD12MUWuOlk5KM7:TR?= NEHoeZdUSU6JRWK=
HUTU-80 NVrvbos{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTxTWM2OD12MUmuNVg2KM7:TR?= NVjpeWhSW0GQR1XS
KNS-42 MmX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWL5SlBXUUN3ME20NlUvQDF3IN88US=> MlLqV2FPT0WU
SH-4 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3SZXExUUN3ME20NlcvPTZ3IN88US=> MnHNV2FPT0WU
L-540 NVfqRXJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnP0TWM2OD12M{GuNFMyKM7:TR?= MmHIV2FPT0WU
NB10 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXyS4JPUUN3ME20OFEvOjN2IN88US=> NEDaW5FUSU6JRWK=
ES1 MkPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LyOGlEPTB;NEWyMlc2OyEQvF2= MV3TRW5ITVJ?
KMOE-2 NWnSNJc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2H1XGlEPTB;NEW2MlcyOSEQvF2= MVrTRW5ITVJ?
MC116 NXvFSm1JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\KXlZKSzVyPUS1PE4yOTZizszN MlPCV2FPT0WU
RCC10RGB Ml3tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnG4TWM2OD12NkCuNFA2KM7:TR?= M2q4d3NCVkeHUh?=
RL95-2 Mlj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYT4Zm5VUUN3ME20OlAvOjN5IN88US=> M37FTXNCVkeHUh?=
Raji M2TFd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXqWllKSzVyPUS2PE4yPDNizszN M3zzbXNCVkeHUh?=
CAS-1 NVG3e|VTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXvbZpKSzVyPUS3Nk4xPzNizszN NGf2bW1USU6JRWK=
Calu-6 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTR5NT6yOlUh|ryP MV\TRW5ITVJ?
KG-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fnXGlEPTB;NEe4MlQ1KM7:TR?= MWHTRW5ITVJ?
LB771-HNC M2nGV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\4THBkUUN3ME20PFIvOjN{IN88US=> NUf1dmg{W0GQR1XS
ACN M2DHNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfoTWM2OD12OUOuOVk6KM7:TR?= MkfXV2FPT0WU
KM12 NIT5bGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkC2TWM2OD12OU[uOVg6KM7:TR?= MUXTRW5ITVJ?

... 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 warming (24.29 mM)
エタノール 2 mg/mL warming (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)

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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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