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 NWDCUXk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoX6TWM2OD13Lki2OlYh|ryP MXvTRW5ITVJ?
DOHH-2 MmCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTlwM{W2PFkh|ryP M4juUHNCVkeHUh?=
no-10 MlftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTlwOUCzPUDPxE1? M2HKPHNCVkeHUh?=
LS-513 NHvtOnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTFzLkO1OFch|ryP MV3TRW5ITVJ?
ALL-PO NHnMZZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTFzLke3N|Qh|ryP MlvxV2FPT0WU
8-MG-BA NXvaWIhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\DNGlEPTB;MUOuNVEzOyEQvF2= M{nCfHNCVkeHUh?=
RPMI-8402 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\YSI1KSzVyPUG1Mlg2OzdizszN NILUVI1USU6JRWK=
EoL-1-cell M13l[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\5TWM2OD1zOD61PVQ5KM7:TR?= M{m2S3NCVkeHUh?=
NALM-6 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfFW3RKSzVyPUG5MlAyPjdizszN MlHyV2FPT0WU
DEL MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTJyLkG0O|Eh|ryP MV7TRW5ITVJ?
SR MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTJ|Lk[3NVUh|ryP MXzTRW5ITVJ?
697 NYnSfIVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\xcWlEPTB;Mk[uOlE2PSEQvF2= MnnSV2FPT0WU
COLO-829 NFjXNI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXIWlRzUUN3ME2yOk45PDh|IN88US=> NIrTNldUSU6JRWK=
EVSA-T M4nscWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXFTWM2OD1{Nz61OVYyKM7:TR?= NFHicmlUSU6JRWK=
ATN-1 M3rYcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXZWYdKSzVyPUOxMlI{OjlizszN MXjTRW5ITVJ?
L-363 NWjW[5VjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1ywe2lEPTB;M{GuO|Q3OSEQvF2= M3;ac3NCVkeHUh?=
LAMA-84 M1L5cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vrc2lEPTB;M{KuOVIyOSEQvF2= M13JfXNCVkeHUh?=
NOS-1 M{nBVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULNTnlWUUN3ME2zOE4zQTV4IN88US=> M{WycXNCVkeHUh?=
BB30-HNC MnTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTN2LkOzNFYh|ryP Mn7mV2FPT0WU
BC-1 M3PSe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTN5Lkm3OFYh|ryP MYDTRW5ITVJ?
IST-SL2 NVP3ZYdoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTN6LkKyOEDPxE1? MnvxV2FPT0WU
D-392MG NUTkN|FoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfOZZdKSzVyPUSwMlIzOTVizszN NHzHdmFUSU6JRWK=
no-11 NV7udYpYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYi4N4p3UUN3ME20NE42PTJzIN88US=> MkjHV2FPT0WU
LC4-1 MkTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWC0flhYUUN3ME20NE45PzF4IN88US=> NXnJO4d1W0GQR1XS
A388 NED1[GdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojoTWM2OD12Mj61PFQ5KM7:TR?= NVT4SmNCW0GQR1XS
NTERA-S-cl-D1 Mo\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTMSZNVUUN3ME20Nk44ODd2IN88US=> NUfSZm1MW0GQR1XS
CESS MkLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDHcJdKSzVyPUS0MlIzOzJizszN M{XtNnNCVkeHUh?=
RS4-11 MmC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\QNmlEPTB;NEmuNFk{QCEQvF2= M3zsUnNCVkeHUh?=
MS-1 M1LvZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjLfY1KSzVyPUWwMlk{PTFizszN M2TR[XNCVkeHUh?=
CTV-1 M4\jOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHaZog3UUN3ME21NU4xPzRizszN M4rkPHNCVkeHUh?=
D-502MG Mn7aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDyTY9UUUN3ME21NU43OjdzIN88US=> M2ra[HNCVkeHUh?=
ML-2 NIL4[IRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTV{LkmxPVUh|ryP Mm\kV2FPT0WU
SK-NEP-1 M1O4[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIL0bHhKSzVyPUWzMlM6OjNizszN Ml\6V2FPT0WU
LOXIMVI MkLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTV|LkW4PFQh|ryP M2rMVHNCVkeHUh?=
DJM-1 MoTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3RTWM2OD13Nj6zN|kyKM7:TR?= MmDCV2FPT0WU
GI-1 NIezVIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7JPHkzUUN3ME21Ok43OTR7IN88US=> M2TIOXNCVkeHUh?=
IST-MES1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M124W2lEPTB;NkCuOVQ6OyEQvF2= MkPtV2FPT0WU
MV-4-11 NVuz[ZdmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV33SoNtUUN3ME22NE43PTN6IN88US=> MX;TRW5ITVJ?
OVCAR-4 M{XHV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TkfWlEPTB;NkOuOVY2PyEQvF2= MUTTRW5ITVJ?
KE-37 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3f0UmlEPTB;Nk[uNlY3QCEQvF2= NXn3NY1JW0GQR1XS
D-542MG MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnH5TWM2OD14OD60NVM2KM7:TR?= MVLTRW5ITVJ?
MHH-PREB-1 NIHZfpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXHW2JvUUN3ME23Nk45PDRzIN88US=> NWT6V2hsW0GQR1XS
MRK-nu-1 NHjCcHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\TeGlEPTB;N{OuOFcxPSEQvF2= M361eHNCVkeHUh?=
D-247MG MmfLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlX5TWM2OD15Mz61OFQzKM7:TR?= MYXTRW5ITVJ?
OCI-AML2 NX\HXGttT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTd4LkmzOlkh|ryP MXzTRW5ITVJ?
LP-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTh{Lki3N|Eh|ryP MlL3V2FPT0WU
HCC1599 M{jaNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fCUGlEPTB;OESuNlg{PyEQvF2= MWrTRW5ITVJ?
KARPAS-45 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7lTWM2OD16ND62PVkzKM7:TR?= M{e1fXNCVkeHUh?=
BE-13 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnBV5NKSzVyPUm5MlA1PzdizszN MWPTRW5ITVJ?
GCIY NEPFTmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\Gb2lEPTB;OUmuNFk2PCEQvF2= M3HwN3NCVkeHUh?=
BV-173 M1zqWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHJTWM2OD1zMECuN|I2KM7:TR?= NIjpdpVUSU6JRWK=
LB2518-MEL M2[2SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHT1Z4ZKSzVyPUGwNE44QDlizszN NInkfm9USU6JRWK=
KS-1 M4Xpcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXYNJVQUUN3ME2xNFEvPjN7IN88US=> MoDIV2FPT0WU
MOLT-16 MoDPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTFyND65PFYh|ryP NI\kV3RUSU6JRWK=
NCI-H1770 NYL2NGkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHuTWM2OD1zMEiuO|g1KM7:TR?= MXrTRW5ITVJ?
NCI-H82 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjNSm97UUN3ME2xNVAvQTd4IN88US=> M1rGUXNCVkeHUh?=
NCCIT MoD0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHLT5dyUUN3ME2xNVIvPTJ7IN88US=> NF\OfHBUSU6JRWK=
KALS-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTFzNT65OFEh|ryP MlSwV2FPT0WU
LB2241-RCC M376S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHSTWM2OD1zMU[uOlc6KM7:TR?= MmGxV2FPT0WU
HH NXq0XZU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzYW2RKSzVyPUGxO{4{QTVizszN M3PVcnNCVkeHUh?=
HD-MY-Z NEHVOXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELXdZJKSzVyPUGxPE41QDhizszN MYrTRW5ITVJ?
EB-3 M{T6fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PvemlEPTB;MUKzMlA6PCEQvF2= MV\TRW5ITVJ?
BL-70 NHPlVZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jjUmlEPTB;MUKzMlEzPyEQvF2= M3;xZ3NCVkeHUh?=
K-562 MnHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWO0doVYUUN3ME2xNlYvOjR3IN88US=> NFPGO4pUSU6JRWK=
HT-144 MkX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3f4dGlEPTB;MUOzMlE3PCEQvF2= NGPCdYNUSU6JRWK=
PF-382 NWfxW4VRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIP5PZVKSzVyPUGzOE4{PjFizszN NF[ycGRUSU6JRWK=
RPMI-8226 MnrsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLwb3lKSzVyPUGzOU4xPDVizszN Mn3IV2FPT0WU
NCI-H1355 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzFTWM2OD1zM{WuOVg4KM7:TR?= NWfzTo51W0GQR1XS
LXF-289 MnjNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX[3ZoY4UUN3ME2xN|kvPzhzIN88US=> NYPFO2hFW0GQR1XS
NCI-H69 M3rNdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LQcGlEPTB;MUSyMlk{OiEQvF2= M{DRNXNCVkeHUh?=
SK-MEL-1 M2D3eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2ezOGlEPTB;MUS3MlE{KM7:TR?= NFv3WYtUSU6JRWK=
KARPAS-299 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXiTWM2OD1zNEmuNVIh|ryP M4j5Z3NCVkeHUh?=
GB-1 NFruV|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Pm[WlEPTB;MUS5MlMzOiEQvF2= NIDpUpBUSU6JRWK=
CMK M4my[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDrTWM2OD1zNEmuOVE2KM7:TR?= MVHTRW5ITVJ?
MPP-89 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHUTWM2OD1zNU[uNFM2KM7:TR?= MXHTRW5ITVJ?
KU812 NV3B[XM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zMc2lEPTB;MU[xMlkxOiEQvF2= M{fzS3NCVkeHUh?=
REH NXu5eYRnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTF4Mj6xNlUh|ryP NV;1V5JGW0GQR1XS
NEC8 NGfYcYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfXTWM2OD1zNkWuNFI3KM7:TR?= M3\nOnNCVkeHUh?=
KP-N-YS MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzFPJlJUUN3ME2xOlgvOzl3IN88US=> MmDGV2FPT0WU
Ramos-2G6-4C10 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\JZVhKSzVyPUG2PU46OTVizszN M4TSS3NCVkeHUh?=
Becker NES2[4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HV[WlEPTB;MUe0MlE5KM7:TR?= NUX2VXlpW0GQR1XS
LB647-SCLC M1Ptd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjRdYVnUUN3ME2xO|UvQDR3IN88US=> M33vWHNCVkeHUh?=
LU-139 NXP2cGdKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHLTWM2OD1zN{iuNFE6KM7:TR?= M{K4THNCVkeHUh?=
QIMR-WIL NGTDVIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7qNmxKSzVyPUG3PU43PDZizszN MoS4V2FPT0WU
NCI-H1395 NVXv[oJiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnjUGJmUUN3ME2xO|kvQTl4IN88US=> NFPkVZhUSU6JRWK=
NOMO-1 M2PnW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\2OW5KSzVyPUG4Nk45PSEQvF2= MoLpV2FPT0WU
GI-ME-N MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LsS2lEPTB;MUi3Mlk3QSEQvF2= NEfkTZNUSU6JRWK=
KMS-12-PE NH;0UHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTF6OT6yO|Mh|ryP NHq1eI9USU6JRWK=
Daudi MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPScopKSzVyPUG5NU4yOjhizszN M4TLZXNCVkeHUh?=
LB996-RCC NVLrUGJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTF7MT62PVkh|ryP MmnCV2FPT0WU
NCI-H2107 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTF7Mz63N|kh|ryP Ml23V2FPT0WU
SK-PN-DW M374XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnW0TWM2OD1zOUSuO|E6KM7:TR?= MnTUV2FPT0WU
MC-CAR NV3xTlRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljLTWM2OD1{MEKuNlU{KM7:TR?= M{nYNXNCVkeHUh?=
SNB75 MlntS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULxdoRyUUN3ME2yNlEvQTRizszN MXTTRW5ITVJ?
ES4 NFHtN2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInsWoxKSzVyPUKyN{44QDNizszN MXTTRW5ITVJ?
KARPAS-422 M33UPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTJ{OD6zOVIh|ryP M1naZnNCVkeHUh?=
NCI-H1648 NIrnXWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlO2TWM2OD1{MkmuOFg6KM7:TR?= MUnTRW5ITVJ?
ES6 NYTQVI9ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXz0TY9CUUN3ME2yN|kvPDNizszN MkDtV2FPT0WU
KNS-81-FD MnzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2X1c2lEPTB;MkSxMlE6PyEQvF2= NV;CeXJFW0GQR1XS
JAR M33oe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PKbmlEPTB;MkW2MlIzPSEQvF2= MUTTRW5ITVJ?
NB1 M{P1Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\KTWM2OD1{NkCuOVE3KM7:TR?= MXvTRW5ITVJ?
D-336MG M3:0N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnvSmF4UUN3ME2yOlAvPjl6IN88US=> M3T2dnNCVkeHUh?=
BC-3 Mn7sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjnSlRwUUN3ME2yOlUvOTd6IN88US=> NV7US2JwW0GQR1XS
HCC2218 M1;6[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PqeGlEPTB;Mk[2MlQyPSEQvF2= NIDsXmxUSU6JRWK=
TE-9 NGe0U4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnm2TWM2OD1{Nk[uOlI4KM7:TR?= NYDjclNCW0GQR1XS
LB1047-RCC Mo[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTJ4Nj63OVMh|ryP MVXTRW5ITVJ?
CTB-1 NVzHbnJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TibWlEPTB;Mk[5Mlk4OyEQvF2= M3;DcXNCVkeHUh?=
NB7 Mlv0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVW2UWEzUUN3ME2yO|Eh|ryP NGHhbWRUSU6JRWK=
ST486 NFzV[4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYP1PWtCUUN3ME2yO|cvPDF{IN88US=> NE[3[VJUSU6JRWK=
HCC1187 NFW5WYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXf3epZ2UUN3ME2yPFIvQDFzIN88US=> NGe3VZdUSU6JRWK=
NCI-SNU-16 MnOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXtSphKSzVyPUK4OE4zPDhizszN M2PtfXNCVkeHUh?=
COR-L279 NUjvS|ZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnWcpBLUUN3ME2yPVEvPTh2IN88US=> NVLZe4R2W0GQR1XS
ES8 NGjzNXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{T6NGlEPTB;Mkm0MlE5OiEQvF2= MnnjV2FPT0WU
U-698-M M2TyOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHaTWM2OD1{OUiuNlQ{KM7:TR?= NHT4XZRUSU6JRWK=
HEL NYjZVYlMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfDTWM2OD1|MEmuNVQ6KM7:TR?= NXq2UYdnW0GQR1XS
KINGS-1 M1PHfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLXTWM2OD1|MUCuOlc1KM7:TR?= MX;TRW5ITVJ?
KY821 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;scI1KSzVyPUOzOk42QTVizszN NWfMVlZTW0GQR1XS
MZ1-PC Mn3NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPFdIxKSzVyPUO0OU43OThizszN MXrTRW5ITVJ?
LS-411N MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFL6fotKSzVyPUO1OE43PiEQvF2= NV7zRXAzW0GQR1XS
SIG-M5 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXS[WZKSzVyPUO1PU44QDJizszN MlXkV2FPT0WU
HT Mn61S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\RT2lEPTB;M{[3MlcyOSEQvF2= NUS2cpRUW0GQR1XS
HC-1 M{\NV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfRTWM2OD1|NkeuO|g4KM7:TR?= NHn1Rm9USU6JRWK=
NCI-H1694 M1LzVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEToWVZKSzVyPUO3Nk46OzRizszN MVnTRW5ITVJ?
BB65-RCC MkniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTqO25qUUN3ME2zO|YvOjR3IN88US=> MoHJV2FPT0WU
HAL-01 M2HLdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTN5OT64N|gh|ryP NH\PNYFUSU6JRWK=
ARH-77 M3yzSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDCOW1KSzVyPUO5OE4xODhizszN MoflV2FPT0WU
MZ7-mel MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTN7Nz6yN|Mh|ryP MnzTV2FPT0WU
SIMA NEC1SmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnmTWM2OD12MEOuPVM{KM7:TR?= NWXKdoJVW0GQR1XS
DG-75 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlT5TWM2OD12MUWuOlk5KM7:TR?= NFzZW2JUSU6JRWK=
HUTU-80 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnWxTWM2OD12MUmuNVg2KM7:TR?= M4npdXNCVkeHUh?=
KNS-42 MljzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjOS5lJUUN3ME20NlUvQDF3IN88US=> M17ldXNCVkeHUh?=
SH-4 M2T4S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTR{Nz61OlUh|ryP NHvWV4lUSU6JRWK=
L-540 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnreoh5UUN3ME20N|EvODNzIN88US=> Ml;hV2FPT0WU
NB10 NGPWVoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLiTWM2OD12NEGuNlM1KM7:TR?= NE\YdolUSU6JRWK=
ES1 NWf0UpB6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXpTWM2OD12NUKuO|U{KM7:TR?= M3SycnNCVkeHUh?=
KMOE-2 NXTufXhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkT5TWM2OD12NU[uO|EyKM7:TR?= MYrTRW5ITVJ?
MC116 M3jOTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYS2dZJnUUN3ME20OVgvOTF4IN88US=> M{D5XXNCVkeHUh?=
RCC10RGB Mmr3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rlWmlEPTB;NE[wMlAxPSEQvF2= M3vBZnNCVkeHUh?=
RL95-2 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGiyWXFKSzVyPUS2NE4zOzdizszN M2X6PXNCVkeHUh?=
Raji NWjieZBuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTR4OD6xOFMh|ryP NX\ITGI{W0GQR1XS
CAS-1 M3PRZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkH1TWM2OD12N{KuNFc{KM7:TR?= MmqxV2FPT0WU
Calu-6 M1PPd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TQTmlEPTB;NEe1MlI3PSEQvF2= NEK0fmFUSU6JRWK=
KG-1 NHrwfGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETad2NKSzVyPUS3PE41PCEQvF2= MluzV2FPT0WU
LB771-HNC NE\JRYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofWTWM2OD12OEKuNlMzKM7:TR?= NIj0U5JUSU6JRWK=
ACN M33xWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTR7Mz61PVkh|ryP MnHhV2FPT0WU
KM12 M4LhZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;JTWM2OD12OU[uOVg6KM7:TR?= MXXTRW5ITVJ?

... 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)-

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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