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 NIro[YdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfOUGJKSzVyPUWuPFY3PiEQvF2= MmPjV2FPT0WU
DOHH-2 M3nTZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFn1dHBKSzVyPUmuN|U3QDlizszN NXzXNYFCW0GQR1XS
no-10 NHT3XXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jub2lEPTB;OT65NFM6KM7:TR?= Ml;zV2FPT0WU
LS-513 M{DGZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPhSmFpUUN3ME2xNU4{PTR5IN88US=> MXrTRW5ITVJ?
ALL-PO M4DLN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1uy[WlEPTB;MUGuO|c{PCEQvF2= MlTkV2FPT0WU
8-MG-BA MkmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1P0SWlEPTB;MUOuNVEzOyEQvF2= MXLTRW5ITVJ?
RPMI-8402 NUXMcYIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvvWXpKSzVyPUG1Mlg2OzdizszN MlKwV2FPT0WU
EoL-1-cell MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfSTWM2OD1zOD61PVQ5KM7:TR?= M4nleXNCVkeHUh?=
NALM-6 M1H0Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3B[VNKSzVyPUG5MlAyPjdizszN M1vJSHNCVkeHUh?=
DEL MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLDVGRKSzVyPUKwMlE1PzFizszN NVX0ZnBFW0GQR1XS
SR M2O5R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTJ|Lk[3NVUh|ryP MW\TRW5ITVJ?
697 MmS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnqVYlKSzVyPUK2MlYyPTVizszN MUPTRW5ITVJ?
COLO-829 NV3JbppvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXT6[5oyUUN3ME2yOk45PDh|IN88US=> M3XVTHNCVkeHUh?=
EVSA-T MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmr4TWM2OD1{Nz61OVYyKM7:TR?= MV3TRW5ITVJ?
ATN-1 M4K0c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHsSGxKSzVyPUOxMlI{OjlizszN NHT0cFNUSU6JRWK=
L-363 M{\vTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnlTWM2OD1|MT63OFYyKM7:TR?= NVXLN2xtW0GQR1XS
LAMA-84 NV74TWNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUD1RWI5UUN3ME2zNk42OjFzIN88US=> MWXTRW5ITVJ?
NOS-1 NYPqcFBNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\UPHdNUUN3ME2zOE4zQTV4IN88US=> MkTaV2FPT0WU
BB30-HNC MoDhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTN2LkOzNFYh|ryP NX23RVV1W0GQR1XS
BC-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4X1bmlEPTB;M{euPVc1PiEQvF2= MlfZV2FPT0WU
IST-SL2 MkPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjJTWM2OD1|OD6yNlQh|ryP NX[3XJlNW0GQR1XS
D-392MG NGr3bIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\2[oJKSzVyPUSwMlIzOTVizszN NWrlVoNIW0GQR1XS
no-11 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTRyLkW1NlEh|ryP MXLTRW5ITVJ?
LC4-1 NUjNWnV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfaSo9HUUN3ME20NE45PzF4IN88US=> NIjCOHRUSU6JRWK=
A388 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTR{LkW4OFgh|ryP NW\wU|NrW0GQR1XS
NTERA-S-cl-D1 NEXYbpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HEUmlEPTB;NEKuO|A4PCEQvF2= Mn3tV2FPT0WU
CESS NH3FSotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nFemlEPTB;NESuNlI{OiEQvF2= NIfU[|NUSU6JRWK=
RS4-11 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjyd|BKSzVyPUS5MlA6OzhizszN NIPCZWJUSU6JRWK=
MS-1 M4\zZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zqUmlEPTB;NUCuPVM2OSEQvF2= M4fDbHNCVkeHUh?=
CTV-1 M3\uZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLYTWM2OD13MT6wO|Qh|ryP M1q0ZnNCVkeHUh?=
D-502MG MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NESxRmhKSzVyPUWxMlYzPzFizszN MWLTRW5ITVJ?
ML-2 NWLMOFlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\xZndKSzVyPUWyMlkyQTVizszN MnTSV2FPT0WU
SK-NEP-1 M1\VVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWD3SXpFUUN3ME21N{4{QTJ|IN88US=> MV;TRW5ITVJ?
LOXIMVI NHnvRZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3ETWM2OD13Mz61PFg1KM7:TR?= MUjTRW5ITVJ?
DJM-1 Mo\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTV4LkOzPVEh|ryP NULBco9xW0GQR1XS
GI-1 NHfyNWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jqWGlEPTB;NU[uOlE1QSEQvF2= MY\TRW5ITVJ?
IST-MES1 NIfWb5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\jZ49mUUN3ME22NE42PDl|IN88US=> MnzRV2FPT0WU
MV-4-11 MlGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkSwTWM2OD14MD62OVM5KM7:TR?= MU\TRW5ITVJ?
OVCAR-4 NWHheZFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDoV3FKSzVyPU[zMlU3PTdizszN M3;t[3NCVkeHUh?=
KE-37 NHHLbndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37lO2lEPTB;Nk[uNlY3QCEQvF2= M{[xc3NCVkeHUh?=
D-542MG MoX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLtWWNKSzVyPU[4MlQyOzVizszN NIXOR2pUSU6JRWK=
MHH-PREB-1 M4fie2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHyT2F6UUN3ME23Nk45PDRzIN88US=> NHXhfmlUSU6JRWK=
MRK-nu-1 NYK3XJVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXnV|d{UUN3ME23N{41PzB3IN88US=> MV;TRW5ITVJ?
D-247MG NFTLcIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnq2TWM2OD15Mz61OFQzKM7:TR?= MorRV2FPT0WU
OCI-AML2 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfvTWM2OD15Nj65N|Y6KM7:TR?= NE\XfGRUSU6JRWK=
LP-1 M1fS[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rRUWlEPTB;OEKuPFc{OSEQvF2= NEW1SZVUSU6JRWK=
HCC1599 NGmyXJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\CWGlEPTB;OESuNlg{PyEQvF2= M4PRZnNCVkeHUh?=
KARPAS-45 M1\FPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnC[FNKSzVyPUi0MlY6QTJizszN NHz1[29USU6JRWK=
BE-13 NHWwcpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofpTWM2OD17OT6wOFc4KM7:TR?= MV;TRW5ITVJ?
GCIY NW\HdoxKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGizdXNKSzVyPUm5MlA6PTRizszN MU\TRW5ITVJ?
BV-173 NEPhV|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1G3RWlEPTB;MUCwMlMzPSEQvF2= MoHwV2FPT0WU
LB2518-MEL MmW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUWzbWZmUUN3ME2xNFAvPzh7IN88US=> MVfTRW5ITVJ?
KS-1 M1fZRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPTNIdKSzVyPUGwNU43OzlizszN MYfTRW5ITVJ?
MOLT-16 M2PSc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3ueXlwUUN3ME2xNFQvQTh4IN88US=> Mo\4V2FPT0WU
NCI-H1770 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYC1cHA1UUN3ME2xNFgvPzh2IN88US=> NX3zfFU{W0GQR1XS
NCI-H82 M{S1bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWS2d|E5UUN3ME2xNVAvQTd4IN88US=> MXjTRW5ITVJ?
NCCIT M{Gxb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmf6TWM2OD1zMUKuOVI6KM7:TR?= M3z2cXNCVkeHUh?=
KALS-1 MmWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvHZ4pJUUN3ME2xNVUvQTRzIN88US=> NXq4UIlwW0GQR1XS
LB2241-RCC NVzpNlR4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTFzNj62O|kh|ryP MkjvV2FPT0WU
HH NEXET5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1P1UWlEPTB;MUG3MlM6PSEQvF2= NVTG[4dUW0GQR1XS
HD-MY-Z MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYH1foQxUUN3ME2xNVgvPDh6IN88US=> NEDM[WZUSU6JRWK=
EB-3 NIXZOmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHpTm9jUUN3ME2xNlMvODl2IN88US=> M1\lOnNCVkeHUh?=
BL-70 NUXyNI5xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVv4WWZHUUN3ME2xNlMvOTJ5IN88US=> MUDTRW5ITVJ?
K-562 MmrlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3W0NmlEPTB;MUK2MlI1PSEQvF2= NH61RYVUSU6JRWK=
HT-144 M4TTUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPpR4JKSzVyPUGzN{4yPjRizszN NITzcYlUSU6JRWK=
PF-382 M2ju[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13QXWlEPTB;MUO0MlM3OSEQvF2= MmP2V2FPT0WU
RPMI-8226 NGTRT|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTF|NT6wOFUh|ryP MoTqV2FPT0WU
NCI-H1355 NI[1UGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTF|NT61PFch|ryP MmPZV2FPT0WU
LXF-289 NISwbJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTF|OT63PFEh|ryP NWizd5lbW0GQR1XS
NCI-H69 M{PuR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTF2Mj65N|Ih|ryP M4W3VXNCVkeHUh?=
SK-MEL-1 NYLj[JlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\LTWM2OD1zNEeuNVMh|ryP MY\TRW5ITVJ?
KARPAS-299 MkDSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;RVHhbUUN3ME2xOFkvOTJizszN NYTyemFsW0GQR1XS
GB-1 Mnj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{n0XWlEPTB;MUS5MlMzOiEQvF2= Mlf5V2FPT0WU
CMK NWTtU29JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\tTWM2OD1zNEmuOVE2KM7:TR?= M374cHNCVkeHUh?=
MPP-89 MmfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTF3Nj6wN|Uh|ryP NGfmWIJUSU6JRWK=
KU812 MlrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGGwUnRKSzVyPUG2NU46ODJizszN M3KxeHNCVkeHUh?=
REH M{G1Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLNNXlKSzVyPUG2Nk4yOjVizszN Mn7mV2FPT0WU
NEC8 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDWRVdKSzVyPUG2OU4xOjZizszN M3rk[3NCVkeHUh?=
KP-N-YS NGDWN4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTF4OD6zPVUh|ryP MnnyV2FPT0WU
Ramos-2G6-4C10 MnfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTF4OT65NVUh|ryP NGLzNVFUSU6JRWK=
Becker NVXYRWtUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTF5ND6xPEDPxE1? Mn7BV2FPT0WU
LB647-SCLC NFvkfpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkL1TWM2OD1zN{WuPFQ2KM7:TR?= NEnxcG1USU6JRWK=
LU-139 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTF5OD6wNVkh|ryP M4HMZ3NCVkeHUh?=
QIMR-WIL NH:zRpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjjWmdKSzVyPUG3PU43PDZizszN MXvTRW5ITVJ?
NCI-H1395 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTBdJRKUUN3ME2xO|kvQTl4IN88US=> MV3TRW5ITVJ?
NOMO-1 MmnzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;TTWM2OD1zOEKuPFUh|ryP NULaVZBCW0GQR1XS
GI-ME-N M1TvbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTF6Nz65Olkh|ryP MVnTRW5ITVJ?
KMS-12-PE M4[5NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWCzcJk3UUN3ME2xPFkvOjd|IN88US=> M1PCTnNCVkeHUh?=
Daudi NIS0S5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17HRmlEPTB;MUmxMlEzQCEQvF2= NILKZoNUSU6JRWK=
LB996-RCC M3X6fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\YTWM2OD1zOUGuOlk6KM7:TR?= NUXYbGlNW0GQR1XS
NCI-H2107 MlH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXSNI1KSzVyPUG5N{44OzlizszN NVPrTXF7W0GQR1XS
SK-PN-DW M{GweGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rRZmlEPTB;MUm0MlcyQSEQvF2= M1HUT3NCVkeHUh?=
MC-CAR NYX4SoNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlW4TWM2OD1{MEKuNlU{KM7:TR?= M{\SWXNCVkeHUh?=
SNB75 MlXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\GSFVKSzVyPUKyNU46PCEQvF2= NGfyZXhUSU6JRWK=
ES4 MoXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3X4RmlEPTB;MkKzMlc5OyEQvF2= MnfhV2FPT0WU
KARPAS-422 MoLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LITGlEPTB;MkK4MlM2OiEQvF2= MYXTRW5ITVJ?
NCI-H1648 NX;3NGdWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7WTWM2OD1{MkmuOFg6KM7:TR?= M3;ofXNCVkeHUh?=
ES6 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTJ|OT60N{DPxE1? MXjTRW5ITVJ?
KNS-81-FD NIXjdJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37sXmlEPTB;MkSxMlE6PyEQvF2= MoLIV2FPT0WU
JAR NHnWVGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnuTWM2OD1{NU[uNlI2KM7:TR?= NHfBSIhUSU6JRWK=
NB1 NWPGSZp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlewTWM2OD1{NkCuOVE3KM7:TR?= NHnWXnhUSU6JRWK=
D-336MG NFHY[JRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTJ4MD62PVgh|ryP MlzUV2FPT0WU
BC-3 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1f2UWlEPTB;Mk[1MlE4QCEQvF2= MlTOV2FPT0WU
HCC2218 NWX6UXlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnk[o57UUN3ME2yOlYvPDF3IN88US=> NUTFPW9{W0GQR1XS
TE-9 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvGc2FvUUN3ME2yOlYvPjJ5IN88US=> NHroOmtUSU6JRWK=
LB1047-RCC MlvWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWmzbVh[UUN3ME2yOlYvPzV|IN88US=> M3XoW3NCVkeHUh?=
CTB-1 M3\lPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlu1TWM2OD1{NkmuPVc{KM7:TR?= MmfuV2FPT0WU
NB7 MkHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfZTWM2OD1{N{Gg{txO MYLTRW5ITVJ?
ST486 M1nQXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTJ5Nz60NVIh|ryP M4nGO3NCVkeHUh?=
HCC1187 MorNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTJ6Mj64NVEh|ryP M3v1O3NCVkeHUh?=
NCI-SNU-16 MoLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fkc2lEPTB;Mki0MlI1QCEQvF2= MnrJV2FPT0WU
COR-L279 MmjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTJ7MT61PFQh|ryP NX;h[GRLW0GQR1XS
ES8 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELm[pZKSzVyPUK5OE4yQDJizszN M2jiU3NCVkeHUh?=
U-698-M M3ixXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjKTWM2OD1{OUiuNlQ{KM7:TR?= NXXJR|EzW0GQR1XS
HEL NVq2ZXVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXKUYNDUUN3ME2zNFkvOTR7IN88US=> NIfNTVZUSU6JRWK=
KINGS-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvUTWM2OD1|MUCuOlc1KM7:TR?= NGWyNnNUSU6JRWK=
KY821 MmXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTN|Nj61PVUh|ryP M3;oVnNCVkeHUh?=
MZ1-PC MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvxWG1KSzVyPUO0OU43OThizszN NI[3TYtUSU6JRWK=
LS-411N M4m4c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmn5TWM2OD1|NUSuOlYh|ryP NVW1b3FkW0GQR1XS
SIG-M5 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXDO5JKSzVyPUO1PU44QDJizszN NFTTbHpUSU6JRWK=
HT M37NUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLOTWM2OD1|NkeuO|EyKM7:TR?= NEDOfINUSU6JRWK=
HC-1 Ml\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV30XHVSUUN3ME2zOlcvPzh5IN88US=> MUHTRW5ITVJ?
NCI-H1694 M2iwOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUS1eFJPUUN3ME2zO|IvQTN2IN88US=> NV31XZZUW0GQR1XS
BB65-RCC NWP5UodoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4CyVGlEPTB;M{e2MlI1PSEQvF2= Mne4V2FPT0WU
HAL-01 MmrkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfjZXl7UUN3ME2zO|kvQDN6IN88US=> M3Ti[XNCVkeHUh?=
ARH-77 NXzqc4k6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHSTYtKSzVyPUO5OE4xODhizszN NE\reXpUSU6JRWK=
MZ7-mel MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFeweFJKSzVyPUO5O{4zOzNizszN NWLmd41RW0GQR1XS
SIMA Mnq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrKd5NTUUN3ME20NFMvQTN|IN88US=> NXLFV3V4W0GQR1XS
DG-75 MnrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;uTGlEPTB;NEG1MlY6QCEQvF2= NYnuZ|hFW0GQR1XS
HUTU-80 M3;6Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;FW2lEPTB;NEG5MlE5PSEQvF2= M4LRW3NCVkeHUh?=
KNS-42 NFnMZ5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXq5UIQ3UUN3ME20NlUvQDF3IN88US=> NIjV[YhUSU6JRWK=
SH-4 NH;MfJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjBPWdKSzVyPUSyO{42PjVizszN M3vwUXNCVkeHUh?=
L-540 NXuzT4FoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTR|MT6wN|Eh|ryP M1fTWXNCVkeHUh?=
NB10 NVzMXlBXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDNTWM2OD12NEGuNlM1KM7:TR?= M37oS3NCVkeHUh?=
ES1 Mkm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{D2[mlEPTB;NEWyMlc2OyEQvF2= Ml;NV2FPT0WU
KMOE-2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILPcnZKSzVyPUS1Ok44OTFizszN MW\TRW5ITVJ?
MC116 NIS0enpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vE[GlEPTB;NEW4MlEyPiEQvF2= MYDTRW5ITVJ?
RCC10RGB MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37KZ2lEPTB;NE[wMlAxPSEQvF2= NF:2RnNUSU6JRWK=
RL95-2 NWfUNI1LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{i2TGlEPTB;NE[wMlI{PyEQvF2= NVfNW5B{W0GQR1XS
Raji M4[5PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfzeoluUUN3ME20OlgvOTR|IN88US=> NWmwVHM{W0GQR1XS
CAS-1 M4rQXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{CwRmlEPTB;NEeyMlA4OyEQvF2= MonHV2FPT0WU
Calu-6 NUDTXWpqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDwZWc3UUN3ME20O|UvOjZ3IN88US=> MoPnV2FPT0WU
KG-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIiwdFZKSzVyPUS3PE41PCEQvF2= MlqwV2FPT0WU
LB771-HNC M37nRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTR6Mj6yN|Ih|ryP MkSxV2FPT0WU
ACN NFLNbpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTR7Mz61PVkh|ryP MXLTRW5ITVJ?
KM12 NYHUV4N6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDkXnRKSzVyPUS5Ok42QDlizszN MY\TRW5ITVJ?

... 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)

技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)

他の質問がある場合は、お気軽くお問合せください。

* 必須

Related ヘッジホッグ/スムーズンド 阻害剤

  • Smoothened Agonist (SAG) HCl

    Smoothened Agonist (SAG) HClは1種の細胞浸透性Smoothened (Smo)の作動剤で、Shh-LIGHT2細胞の中でEC50 値は3 nMです。

  • SB225002

    SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.

  • SB-334867

    SB-334867 is a selective orexin-1 (OX1) receptor antagonist.

  • BAF312 (Siponimod)

    BAF312 (Siponimod) is a next-generation S1P receptor modulator, selective for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, respectively.

  • Vismodegib (GDC-0449)

    Vismodegib (GDC-0449)は、強力で、新しくて、特定のハリネズミ経路阻害剤で、 IC50 が 3 nMになる。

  • GANT61

    GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.

  • Purmorphamine

    Purmorphamine, which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM and also is an inducer of osteoblast differentiation with EC50 of 1 μM.

  • LDE225 (NVP-LDE225,Erismodegib)

    LDE225 (NVP-LDE225,Erismodegib)は、スムーズにされた 敵対者で、IC50 がそれぞれ 1.3 nM (mouse)と 2.5 nM (human)です。

  • Taladegib (LY2940680)

    Taladegib (LY2940680)はSmoレセプターと結合して、強力にHhシグナリングを妨げます。

最近チェックしたアイテム

Tags: Cyclopamineを買う | Cyclopamine供給者 | Cyclopamineを購入する | Cyclopamine費用 | Cyclopamine生産者 | オーダーCyclopamine | Cyclopamine代理店
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
お問い合わせ