Cyclopamine

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。

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電話番号: + 81 3-5632-9610mail@cosmobio.co.jp

Cyclopamine 化学構造
分子量: 411.62

高品質保証

カスタマーフィードバック(4)

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 NG\VSopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LQb2lEPTB;NT64OlY3KM7:TR?= Ml31V2FPT0WU
DOHH-2 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTlwM{W2PFkh|ryP NY\aVmNsW0GQR1XS
no-10 NGTkb4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDufm1KSzVyPUmuPVA{QSEQvF2= M1PPbXNCVkeHUh?=
LS-513 NF:we4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIC2dHNKSzVyPUGxMlM2PDdizszN NVPsfYlxW0GQR1XS
ALL-PO NVfXPHFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fOTWlEPTB;MUGuO|c{PCEQvF2= MXvTRW5ITVJ?
8-MG-BA NVTmVmR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTF|LkGxNlMh|ryP MXjTRW5ITVJ?
RPMI-8402 NVXG[ZV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fmcWlEPTB;MUWuPFU{PyEQvF2= MX3TRW5ITVJ?
EoL-1-cell NGSycZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjmVJZKSzVyPUG4MlU6PDhizszN MYPTRW5ITVJ?
NALM-6 M4rZeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvn[nZSUUN3ME2xPU4xOTZ5IN88US=> M2HLOnNCVkeHUh?=
DEL NUn5UmtlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DhdWlEPTB;MkCuNVQ4OSEQvF2= Mn7JV2FPT0WU
SR NYPlVJQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrs[Y1KSzVyPUKzMlY4OTVizszN NELTdotUSU6JRWK=
697 NVPqPJBWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkK1TWM2OD1{Nj62NVU2KM7:TR?= MmLDV2FPT0WU
COLO-829 M{fkT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTJ4Lki0PFMh|ryP NGG0[IVUSU6JRWK=
EVSA-T M1rydGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPCcZVKSzVyPUK3MlU2PjFizszN M{nufnNCVkeHUh?=
ATN-1 NU\OeohQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7NTWM2OD1|MT6yN|I6KM7:TR?= NV;YUoo6W0GQR1XS
L-363 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4ixVWlEPTB;M{GuO|Q3OSEQvF2= NIDacGVUSU6JRWK=
LAMA-84 NHX0RYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;C[5R2UUN3ME2zNk42OjFzIN88US=> M{W3OXNCVkeHUh?=
NOS-1 NGPDVWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGH0bHdKSzVyPUO0MlI6PTZizszN M3XaZnNCVkeHUh?=
BB30-HNC MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTN2LkOzNFYh|ryP NWK0T3hMW0GQR1XS
BC-1 NIPO[oJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nEc2lEPTB;M{euPVc1PiEQvF2= MV3TRW5ITVJ?
IST-SL2 MkX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jrPGlEPTB;M{iuNlI1KM7:TR?= MYfTRW5ITVJ?
D-392MG MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jCUGlEPTB;NECuNlIyPSEQvF2= NVXnfoJ[W0GQR1XS
no-11 Mk\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETxbXpKSzVyPUSwMlU2OjFizszN Ml65V2FPT0WU
LC4-1 MnHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjUNmZKSzVyPUSwMlg4OTZizszN MmrDV2FPT0WU
A388 NILiSHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTR{LkW4OFgh|ryP NF\VW5BUSU6JRWK=
NTERA-S-cl-D1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXezNWw2UUN3ME20Nk44ODd2IN88US=> MUfTRW5ITVJ?
CESS NE\HVm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4X0dGlEPTB;NESuNlI{OiEQvF2= MV;TRW5ITVJ?
RS4-11 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnGwTWM2OD12OT6wPVM5KM7:TR?= Mk[4V2FPT0WU
MS-1 NEX5dI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTVyLkmzOVEh|ryP NHLUNmlUSU6JRWK=
CTV-1 M4\McGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrmeGdKSzVyPUWxMlA4PCEQvF2= M4P0dnNCVkeHUh?=
D-502MG NWG1T4pQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEGxXohKSzVyPUWxMlYzPzFizszN NEKzWFlUSU6JRWK=
ML-2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\qOmlEPTB;NUKuPVE6PSEQvF2= NUDP[nY{W0GQR1XS
SK-NEP-1 NVj6ZppZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmKyTWM2OD13Mz6zPVI{KM7:TR?= NVr0OJBqW0GQR1XS
LOXIMVI NXrsT5NVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTV|LkW4PFQh|ryP MoPmV2FPT0WU
DJM-1 NELY[WdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HacWlEPTB;NU[uN|M6OSEQvF2= MULTRW5ITVJ?
GI-1 M4PORWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTV4Lk[xOFkh|ryP NXzkTYVjW0GQR1XS
IST-MES1 NE\XfpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVyxUnI6UUN3ME22NE42PDl|IN88US=> Mm\rV2FPT0WU
MV-4-11 NWfhOY55T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13tZ2lEPTB;NkCuOlU{QCEQvF2= MoH2V2FPT0WU
OVCAR-4 NUPkZ495T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\XZoZDUUN3ME22N{42PjV5IN88US=> NF3LR2RUSU6JRWK=
KE-37 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnGTWM2OD14Nj6yOlY5KM7:TR?= Ml\VV2FPT0WU
D-542MG NV31PIpMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3HTWM2OD14OD60NVM2KM7:TR?= NELtSWJUSU6JRWK=
MHH-PREB-1 NEj0[mpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXUe4lXUUN3ME23Nk45PDRzIN88US=> NWDi[oZXW0GQR1XS
MRK-nu-1 NX;hdGtNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3TXYpKSzVyPUezMlQ4ODVizszN MVPTRW5ITVJ?
D-247MG MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTd|LkW0OFIh|ryP NVnoXXVNW0GQR1XS
OCI-AML2 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXW0c2hWUUN3ME23Ok46OzZ7IN88US=> NXnmUGtiW0GQR1XS
LP-1 NGjTUmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTh{Lki3N|Eh|ryP NH7wUXJUSU6JRWK=
HCC1599 MmXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTh2LkK4N|ch|ryP NHT5NXRUSU6JRWK=
KARPAS-45 Mmi5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTh2Lk[5PVIh|ryP M2rKSnNCVkeHUh?=
BE-13 NEnEOZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTl7LkC0O|ch|ryP M1zzZnNCVkeHUh?=
GCIY MkXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmX3TWM2OD17OT6wPVU1KM7:TR?= Mo\TV2FPT0WU
BV-173 M2nWV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjy[I12UUN3ME2xNFAvOzJ3IN88US=> NF7EbXlUSU6JRWK=
LB2518-MEL Mn3GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDr[YpWUUN3ME2xNFAvPzh7IN88US=> MnrFV2FPT0WU
KS-1 NV7idpJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HG[WlEPTB;MUCxMlY{QSEQvF2= M{m4RnNCVkeHUh?=
MOLT-16 NHXIXo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jybWlEPTB;MUC0Mlk5PiEQvF2= M1PvOXNCVkeHUh?=
NCI-H1770 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3rPZBKSzVyPUGwPE44QDRizszN M{KxcXNCVkeHUh?=
NCI-H82 M2PONWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XSRmlEPTB;MUGwMlk4PiEQvF2= NFvOeG9USU6JRWK=
NCCIT NEn6e2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzmWGV2UUN3ME2xNVIvPTJ7IN88US=> MlXrV2FPT0WU
KALS-1 M{PVe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPq[VJ4UUN3ME2xNVUvQTRzIN88US=> MYDTRW5ITVJ?
LB2241-RCC MlvHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHWdZY3UUN3ME2xNVYvPjd7IN88US=> MljHV2FPT0WU
HH MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDhfZJuUUN3ME2xNVcvOzl3IN88US=> NGmyOG9USU6JRWK=
HD-MY-Z MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTFzOD60PFgh|ryP Mk[zV2FPT0WU
EB-3 M13jZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTF{Mz6wPVQh|ryP MnnIV2FPT0WU
BL-70 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkC3TWM2OD1zMkOuNVI4KM7:TR?= M{DYOnNCVkeHUh?=
K-562 NIPhU|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrrTWM2OD1zMk[uNlQ2KM7:TR?= NYPB[ZRyW0GQR1XS
HT-144 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjBRXQ6UUN3ME2xN|MvOTZ2IN88US=> M33E[3NCVkeHUh?=
PF-382 NW[zfXhXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXrZo9YUUN3ME2xN|QvOzZzIN88US=> MVjTRW5ITVJ?
RPMI-8226 MnfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTpV|VGUUN3ME2xN|UvODR3IN88US=> M1HMeXNCVkeHUh?=
NCI-H1355 NYO2Z2xvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTF|NT61PFch|ryP MWPTRW5ITVJ?
LXF-289 MkWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fJSmlEPTB;MUO5Mlc5OSEQvF2= NVTw[G5MW0GQR1XS
NCI-H69 M2S1Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jIdGlEPTB;MUSyMlk{OiEQvF2= MVjTRW5ITVJ?
SK-MEL-1 NX3VdmhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTF2Nz6xN{DPxE1? MYHTRW5ITVJ?
KARPAS-299 NFHYR4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nMTGlEPTB;MUS5MlEzKM7:TR?= MV7TRW5ITVJ?
GB-1 NV33VFI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTF2OT6zNlIh|ryP M4LoU3NCVkeHUh?=
CMK NXjISW9yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\j[plKSzVyPUG0PU42OTVizszN MkPvV2FPT0WU
MPP-89 NE\IbIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXhfmxKSzVyPUG1Ok4xOzVizszN MYHTRW5ITVJ?
KU812 MmqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTF4MT65NFIh|ryP M{TWN3NCVkeHUh?=
REH NEnLToZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLxdGVKSzVyPUG2Nk4yOjVizszN MX7TRW5ITVJ?
NEC8 M3jRWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTF4NT6wNlYh|ryP NIH4[IdUSU6JRWK=
KP-N-YS MmLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LXUmlEPTB;MU[4MlM6PSEQvF2= MWjTRW5ITVJ?
Ramos-2G6-4C10 NEPnfXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LhcmlEPTB;MU[5MlkyPSEQvF2= NUPmWVlvW0GQR1XS
Becker MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLmTWM2OD1zN{SuNVgh|ryP NHiyOFZUSU6JRWK=
LB647-SCLC NV:5O45bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvZTWM2OD1zN{WuPFQ2KM7:TR?= MknRV2FPT0WU
LU-139 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXq5SoFZUUN3ME2xO|gvODF7IN88US=> M{TOcXNCVkeHUh?=
QIMR-WIL M3PsWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LidGlEPTB;MUe5MlY1PiEQvF2= NHrCNGhUSU6JRWK=
NCI-H1395 NI\6dG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTF5OT65PVYh|ryP NX;RcpBkW0GQR1XS
NOMO-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPwTWM2OD1zOEKuPFUh|ryP NGi0VXZUSU6JRWK=
GI-ME-N NXvKV3l2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTF6Nz65Olkh|ryP M2jNdnNCVkeHUh?=
KMS-12-PE M4PxeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3TN5l6UUN3ME2xPFkvOjd|IN88US=> M1LhW3NCVkeHUh?=
Daudi M1HYdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTU[29OUUN3ME2xPVEvOTJ6IN88US=> NF70PYZUSU6JRWK=
LB996-RCC MkLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnqSGtyUUN3ME2xPVEvPjl7IN88US=> NES2WGNUSU6JRWK=
NCI-H2107 M{\xXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4myPWlEPTB;MUmzMlc{QSEQvF2= M13YcXNCVkeHUh?=
SK-PN-DW M1LScGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWj2SXlFUUN3ME2xPVQvPzF7IN88US=> MmP1V2FPT0WU
MC-CAR NFf1Z4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEOyNVlKSzVyPUKwNk4zPTNizszN MWDTRW5ITVJ?
SNB75 M2nCcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYWwRW9GUUN3ME2yNlEvQTRizszN Ml\WV2FPT0WU
ES4 MlvFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3SWINKUUN3ME2yNlMvPzh|IN88US=> M{HsbnNCVkeHUh?=
KARPAS-422 M2n6PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfHdWZKSzVyPUKyPE4{PTJizszN MVvTRW5ITVJ?
NCI-H1648 NFOyPZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPMTWM2OD1{MkmuOFg6KM7:TR?= M1faZXNCVkeHUh?=
ES6 NFuxcHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTJ|OT60N{DPxE1? NIrHVJpUSU6JRWK=
KNS-81-FD M1TKS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DsN2lEPTB;MkSxMlE6PyEQvF2= NUmyRY9VW0GQR1XS
JAR MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvFTllJUUN3ME2yOVYvOjJ3IN88US=> M4\kSXNCVkeHUh?=
NB1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHYZmp[UUN3ME2yOlAvPTF4IN88US=> MX;TRW5ITVJ?
D-336MG MnPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTJ4MD62PVgh|ryP NWGzPHpLW0GQR1XS
BC-3 M3ezVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rHZ2lEPTB;Mk[1MlE4QCEQvF2= M4CyenNCVkeHUh?=
HCC2218 NX3UN3ExT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTJ4Nj60NVUh|ryP MnzjV2FPT0WU
TE-9 NUHQZotRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\Ie2lEPTB;Mk[2MlYzPyEQvF2= MWHTRW5ITVJ?
LB1047-RCC M{LlRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLwbXFKSzVyPUK2Ok44PTNizszN NFfSW29USU6JRWK=
CTB-1 NF7QWnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTJ4OT65O|Mh|ryP M4PaWXNCVkeHUh?=
NB7 NHzIeFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHTOpNwUUN3ME2yO|Eh|ryP Mn7KV2FPT0WU
ST486 NUTBXGtuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnmzTWM2OD1{N{euOFEzKM7:TR?= MV\TRW5ITVJ?
HCC1187 M2PYNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrIPHdKSzVyPUK4Nk45OTFizszN M172OXNCVkeHUh?=
NCI-SNU-16 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7LSVBKSzVyPUK4OE4zPDhizszN NXzVVGJkW0GQR1XS
COR-L279 M3i0Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTyTWM2OD1{OUGuOVg1KM7:TR?= NInUOIRUSU6JRWK=
ES8 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTJ7ND6xPFIh|ryP NGDaVXhUSU6JRWK=
U-698-M MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3IbIxWUUN3ME2yPVgvOjR|IN88US=> MkXvV2FPT0WU
HEL NHO0U21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXsU2ZKSzVyPUOwPU4yPDlizszN NFTXNmhUSU6JRWK=
KINGS-1 M{SwRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPUTWM2OD1|MUCuOlc1KM7:TR?= NXnxSZZQW0GQR1XS
KY821 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVG3dWZsUUN3ME2zN|YvPTl3IN88US=> M{T1VHNCVkeHUh?=
MZ1-PC M1LHcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTN2NT62NVgh|ryP NWDWZZdWW0GQR1XS
LS-411N NWK3UmRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mki4TWM2OD1|NUSuOlYh|ryP MlnWV2FPT0WU
SIG-M5 Mme2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;pXWlEPTB;M{W5Mlc5OiEQvF2= MmrlV2FPT0WU
HT NWrHT|lrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NID3TlJKSzVyPUO2O{44OTFizszN NILHPY9USU6JRWK=
HC-1 NWTkRY42T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\mTWM2OD1|NkeuO|g4KM7:TR?= MojTV2FPT0WU
NCI-H1694 NGL2TIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\NN|ZSUUN3ME2zO|IvQTN2IN88US=> MnXuV2FPT0WU
BB65-RCC MlfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jrN2lEPTB;M{e2MlI1PSEQvF2= MWrTRW5ITVJ?
HAL-01 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PxVGlEPTB;M{e5Mlg{QCEQvF2= NUm4d5dWW0GQR1XS
ARH-77 NFXiUXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjEOohKSzVyPUO5OE4xODhizszN NXz3UZZXW0GQR1XS
MZ7-mel NIW3VmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTN7Nz6yN|Mh|ryP NFPPNnJUSU6JRWK=
SIMA M3;kZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rXbWlEPTB;NECzMlk{OyEQvF2= NIDXOm5USU6JRWK=
DG-75 NFrpT2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDpTWM2OD12MUWuOlk5KM7:TR?= MXrTRW5ITVJ?
HUTU-80 NIfhNGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTRzOT6xPFUh|ryP MlLPV2FPT0WU
KNS-42 Mn\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTs[YZLUUN3ME20NlUvQDF3IN88US=> M1vDb3NCVkeHUh?=
SH-4 NVS2WnNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDWcGd3UUN3ME20NlcvPTZ3IN88US=> NUX2[2xWW0GQR1XS
L-540 NYKzWGxuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnm0TWM2OD12M{GuNFMyKM7:TR?= NIK4ZYhUSU6JRWK=
NB10 NU\pN2J3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTPSm1KSzVyPUS0NU4zOzRizszN NYr2epVrW0GQR1XS
ES1 NVv1[m14T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfFTWM2OD12NUKuO|U{KM7:TR?= M1rQfXNCVkeHUh?=
KMOE-2 M4DWT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvVeYlFUUN3ME20OVYvPzFzIN88US=> NHfYbVlUSU6JRWK=
MC116 Mmm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkCxTWM2OD12NUiuNVE3KM7:TR?= NF;abmpUSU6JRWK=
RCC10RGB NV21bIdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDCSlV2UUN3ME20OlAvODB3IN88US=> MVPTRW5ITVJ?
RL95-2 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfuTWM2OD12NkCuNlM4KM7:TR?= MVHTRW5ITVJ?
Raji MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HXVWlEPTB;NE[4MlE1OyEQvF2= M365UXNCVkeHUh?=
CAS-1 M4jmcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTR5Mj6wO|Mh|ryP M2\xPHNCVkeHUh?=
Calu-6 MkHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWqz[nZVUUN3ME20O|UvOjZ3IN88US=> M2j3OHNCVkeHUh?=
KG-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTR5OD60OEDPxE1? M3:x[nNCVkeHUh?=
LB771-HNC MkTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXVRYRVUUN3ME20PFIvOjN{IN88US=> MXjTRW5ITVJ?
ACN NWnwdoZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXVUZdHUUN3ME20PVMvPTl7IN88US=> NHPHZWpUSU6JRWK=
KM12 MlzXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LwWmlEPTB;NEm2MlU5QSEQvF2= MYXTRW5ITVJ?

... 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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