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 NYTGV2VRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIG2bopKSzVyPUWuPFY3PiEQvF2= M173RnNCVkeHUh?=
DOHH-2 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\KV2lEPTB;OT6zOVY5QSEQvF2= Moe0V2FPT0WU
no-10 NEX5N|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfITWM2OD17LkmwN|kh|ryP M2XNfHNCVkeHUh?=
LS-513 NGjmR25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPp[ppNUUN3ME2xNU4{PTR5IN88US=> Moj0V2FPT0WU
ALL-PO NETjZ2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTFzLke3N|Qh|ryP NHfEV3NUSU6JRWK=
8-MG-BA MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXP2XlBXUUN3ME2xN{4yOTJ|IN88US=> NYTxd4NQW0GQR1XS
RPMI-8402 NUPn[4x6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTF3Lki1N|ch|ryP NHvyVXhUSU6JRWK=
EoL-1-cell NYjQTFk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvxbnNKSzVyPUG4MlU6PDhizszN M1fqfXNCVkeHUh?=
NALM-6 MlG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPucJJ3UUN3ME2xPU4xOTZ5IN88US=> Mof3V2FPT0WU
DEL M1O2[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTJyLkG0O|Eh|ryP NH\0V|JUSU6JRWK=
SR MnTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTJ|Lk[3NVUh|ryP M{\3dHNCVkeHUh?=
697 M4HWdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlT6TWM2OD1{Nj62NVU2KM7:TR?= NX7pcFZHW0GQR1XS
COLO-829 NETIe5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\oXZFKSzVyPUK2Mlg1QDNizszN Mk\SV2FPT0WU
EVSA-T NG\XeXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjEPIpPUUN3ME2yO{42PTZzIN88US=> MXrTRW5ITVJ?
ATN-1 NWXR[VRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;oPWlEPTB;M{GuNlMzQSEQvF2= NYjxdFJ{W0GQR1XS
L-363 MnvBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlS1TWM2OD1|MT63OFYyKM7:TR?= MV\TRW5ITVJ?
LAMA-84 NHn2dFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTN{LkWyNVEh|ryP NFHHUWFUSU6JRWK=
NOS-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfDTWM2OD1|ND6yPVU3KM7:TR?= M{nPXXNCVkeHUh?=
BB30-HNC NYLDblRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PTbmlEPTB;M{SuN|MxPiEQvF2= MYrTRW5ITVJ?
BC-1 NXm4fFBjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moq4TWM2OD1|Nz65O|Q3KM7:TR?= M3OxWnNCVkeHUh?=
IST-SL2 NGrIW4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETWcXBKSzVyPUO4MlIzPCEQvF2= MVTTRW5ITVJ?
D-392MG NXvIRm9LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37YSWlEPTB;NECuNlIyPSEQvF2= M1zObXNCVkeHUh?=
no-11 Mk\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTRyLkW1NlEh|ryP NVTtWnRjW0GQR1XS
LC4-1 MkTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHITWM2OD12MD64O|E3KM7:TR?= NW\wPGdxW0GQR1XS
A388 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37RS2lEPTB;NEKuOVg1QCEQvF2= M32zO3NCVkeHUh?=
NTERA-S-cl-D1 MlfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\xTWM2OD12Mj63NFc1KM7:TR?= NWLYUWVbW0GQR1XS
CESS M4XuVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHzXGdKSzVyPUS0MlIzOzJizszN MW\TRW5ITVJ?
RS4-11 NX\CPZRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDQenhMUUN3ME20PU4xQTN6IN88US=> NUP2VWkxW0GQR1XS
MS-1 NVW0Z5lZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnm1TWM2OD13MD65N|UyKM7:TR?= NXL3[ZhlW0GQR1XS
CTV-1 MmTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rBU2lEPTB;NUGuNFc1KM7:TR?= NIm1UGJUSU6JRWK=
D-502MG M134Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTBWYZ[UUN3ME21NU43OjdzIN88US=> NVW4eXRFW0GQR1XS
ML-2 NITy[2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTV{LkmxPVUh|ryP M4jWbnNCVkeHUh?=
SK-NEP-1 Moj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTV|LkO5NlMh|ryP NV\5eYx3W0GQR1XS
LOXIMVI NVzVUZpyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\G[WNFUUN3ME21N{42QDh2IN88US=> MXvTRW5ITVJ?
DJM-1 NYHpV2pmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDJOG1KSzVyPUW2MlM{QTFizszN M{PJR3NCVkeHUh?=
GI-1 Ml7iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTV4Lk[xOFkh|ryP MYHTRW5ITVJ?
IST-MES1 Mnv0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGqyVIRKSzVyPU[wMlU1QTNizszN M2fiUnNCVkeHUh?=
MV-4-11 M1v6dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTZyLk[1N|gh|ryP NYDrcXdWW0GQR1XS
OVCAR-4 M{LhWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWT4WYFiUUN3ME22N{42PjV5IN88US=> NYe4[plkW0GQR1XS
KE-37 MmnhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLvTWM2OD14Nj6yOlY5KM7:TR?= NGOzPZZUSU6JRWK=
D-542MG Ml\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmqyTWM2OD14OD60NVM2KM7:TR?= M4rQVHNCVkeHUh?=
MHH-PREB-1 M33PS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XNdWlEPTB;N{KuPFQ1OSEQvF2= MmXIV2FPT0WU
MRK-nu-1 NVXNbJd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWO2OIRCUUN3ME23N{41PzB3IN88US=> MXHTRW5ITVJ?
D-247MG MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrQbHQ4UUN3ME23N{42PDR{IN88US=> M{n1SHNCVkeHUh?=
OCI-AML2 NF3ofY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrJ[HRKSzVyPUe2Mlk{PjlizszN NX;nZlF4W0GQR1XS
LP-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTh{Lki3N|Eh|ryP NWTHNFV2W0GQR1XS
HCC1599 NGjyS2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1:0PGlEPTB;OESuNlg{PyEQvF2= MnTHV2FPT0WU
KARPAS-45 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYH4PIc1UUN3ME24OE43QTl{IN88US=> MVvTRW5ITVJ?
BE-13 MoLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrLTWM2OD17OT6wOFc4KM7:TR?= Mn\kV2FPT0WU
GCIY NEnaOZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LKfGlEPTB;OUmuNFk2PCEQvF2= NVPDT2pyW0GQR1XS
BV-173 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3FTWM2OD1zMECuN|I2KM7:TR?= MnXKV2FPT0WU
LB2518-MEL MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\Kc5VKSzVyPUGwNE44QDlizszN MmHiV2FPT0WU
KS-1 MlnOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHacldVUUN3ME2xNFEvPjN7IN88US=> M1i0bHNCVkeHUh?=
MOLT-16 Ml:zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vDdWlEPTB;MUC0Mlk5PiEQvF2= M3H4fXNCVkeHUh?=
NCI-H1770 M4DCe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXuZ2NKSzVyPUGwPE44QDRizszN M1XNXXNCVkeHUh?=
NCI-H82 NIL0OmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTFzMD65O|Yh|ryP NYjT[Y9JW0GQR1XS
NCCIT MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2n3[GlEPTB;MUGyMlUzQSEQvF2= NX\vTXBtW0GQR1XS
KALS-1 NYnjTXRmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXWTWM2OD1zMUWuPVQyKM7:TR?= MmHFV2FPT0WU
LB2241-RCC MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HWR2lEPTB;MUG2MlY4QSEQvF2= NHv0e2pUSU6JRWK=
HH NUH0[nZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\5ZmlEPTB;MUG3MlM6PSEQvF2= M4rGeXNCVkeHUh?=
HD-MY-Z MljGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3xcIM6UUN3ME2xNVgvPDh6IN88US=> MmrJV2FPT0WU
EB-3 NG\IeGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvwTWM2OD1zMkOuNFk1KM7:TR?= NIK5[mNUSU6JRWK=
BL-70 MonDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\0cWlEPTB;MUKzMlEzPyEQvF2= M4HBXnNCVkeHUh?=
K-562 NIrE[|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTF{Nj6yOFUh|ryP M{Kxe3NCVkeHUh?=
HT-144 Moe0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTF|Mz6xOlQh|ryP MYXTRW5ITVJ?
PF-382 NXfpNmhTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTrcYxKSzVyPUGzOE4{PjFizszN NYPNUo9IW0GQR1XS
RPMI-8226 MlfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLSXZJKSzVyPUGzOU4xPDVizszN M2ThbHNCVkeHUh?=
NCI-H1355 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTF|NT61PFch|ryP NFPYbXpUSU6JRWK=
LXF-289 MoPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\rT5B5UUN3ME2xN|kvPzhzIN88US=> NVfRXok2W0GQR1XS
NCI-H69 MmLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfuenJKSzVyPUG0Nk46OzJizszN Mon1V2FPT0WU
SK-MEL-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjZ[JZzUUN3ME2xOFcvOTNizszN MUnTRW5ITVJ?
KARPAS-299 MnHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\id|ZKSzVyPUG0PU4yOiEQvF2= M2frTHNCVkeHUh?=
GB-1 NVLJXWFFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHmyb2tKSzVyPUG0PU4{OjJizszN NVjlW3VRW0GQR1XS
CMK Ml20S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3wTWM2OD1zNEmuOVE2KM7:TR?= NFzTXoxUSU6JRWK=
MPP-89 MnXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTPXodWUUN3ME2xOVYvODN3IN88US=> MXjTRW5ITVJ?
KU812 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTF4MT65NFIh|ryP M17WSHNCVkeHUh?=
REH MkfuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULrcFM5UUN3ME2xOlIvOTJ3IN88US=> NE\GVoFUSU6JRWK=
NEC8 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfhcXpKSzVyPUG2OU4xOjZizszN MonIV2FPT0WU
KP-N-YS NFzwWWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTF4OD6zPVUh|ryP MUPTRW5ITVJ?
Ramos-2G6-4C10 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDRPHN2UUN3ME2xOlkvQTF3IN88US=> NFjlcolUSU6JRWK=
Becker NH;BS2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPWTWM2OD1zN{SuNVgh|ryP NVOxUVNtW0GQR1XS
LB647-SCLC NF6yZ4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLQSVRtUUN3ME2xO|UvQDR3IN88US=> NVvU[o1[W0GQR1XS
LU-139 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLMTpdZUUN3ME2xO|gvODF7IN88US=> MmizV2FPT0WU
QIMR-WIL M2D2[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nlcmlEPTB;MUe5MlY1PiEQvF2= NUi0WmF1W0GQR1XS
NCI-H1395 NGfZZ25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTF5OT65PVYh|ryP NUnsNIxlW0GQR1XS
NOMO-1 M4XLbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTF6Mj64OUDPxE1? NIK0dpNUSU6JRWK=
GI-ME-N M1S0SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTF6Nz65Olkh|ryP NELwXFRUSU6JRWK=
KMS-12-PE Ml\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\UVWlEPTB;MUi5MlI4OyEQvF2= NXG2eVFMW0GQR1XS
Daudi MlzLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rtZWlEPTB;MUmxMlEzQCEQvF2= NIrBe2ZUSU6JRWK=
LB996-RCC M1LEV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPhfVFKSzVyPUG5NU43QTlizszN MnW0V2FPT0WU
NCI-H2107 M2rZOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTF7Mz63N|kh|ryP NUTUc4JtW0GQR1XS
SK-PN-DW MlLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknLTWM2OD1zOUSuO|E6KM7:TR?= MoXMV2FPT0WU
MC-CAR MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGq3N2RKSzVyPUKwNk4zPTNizszN M2PtWnNCVkeHUh?=
SNB75 M1mwemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEH2RopKSzVyPUKyNU46PCEQvF2= NV64NJVbW0GQR1XS
ES4 NEnmb4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2riVmlEPTB;MkKzMlc5OyEQvF2= M3nEPHNCVkeHUh?=
KARPAS-422 NVPueINvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTJ{OD6zOVIh|ryP MUDTRW5ITVJ?
NCI-H1648 NE\EbXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLmc|hFUUN3ME2yNlkvPDh7IN88US=> Mn\2V2FPT0WU
ES6 MljaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37GOWlEPTB;MkO5MlQ{KM7:TR?= NYm5fGxTW0GQR1XS
KNS-81-FD MnvhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrtd|ZKSzVyPUK0NU4yQTdizszN NGrLZYVUSU6JRWK=
JAR NYHkSXRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\xTWlEPTB;MkW2MlIzPSEQvF2= NYTweogyW0GQR1XS
NB1 Ml3NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3qxemlEPTB;Mk[wMlUyPiEQvF2= M{C0VHNCVkeHUh?=
D-336MG MlLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;STWM2OD1{NkCuOlk5KM7:TR?= NVmzWVVbW0GQR1XS
BC-3 NH7l[GJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfoTWM2OD1{NkWuNVc5KM7:TR?= NWLpcFhrW0GQR1XS
HCC2218 M3HjOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFO4Z5ZKSzVyPUK2Ok41OTVizszN NYTCNmUxW0GQR1XS
TE-9 NInsTWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIW1dHhKSzVyPUK2Ok43OjdizszN M1HsenNCVkeHUh?=
LB1047-RCC NU\vblZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfhRZRKSzVyPUK2Ok44PTNizszN M{j4XXNCVkeHUh?=
CTB-1 MljKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rhUmlEPTB;Mk[5Mlk4OyEQvF2= Ml\xV2FPT0WU
NB7 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHSS2pKSzVyPUK3NUDPxE1? NFuyV4lUSU6JRWK=
ST486 NEW1V2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTZZlV1UUN3ME2yO|cvPDF{IN88US=> M4CzZ3NCVkeHUh?=
HCC1187 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fpVGlEPTB;MkiyMlgyOSEQvF2= MlzqV2FPT0WU
NCI-SNU-16 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHrTWM2OD1{OESuNlQ5KM7:TR?= M2rnRnNCVkeHUh?=
COR-L279 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7SXmk{UUN3ME2yPVEvPTh2IN88US=> Mny1V2FPT0WU
ES8 NH3mXGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHjTWM2OD1{OUSuNVgzKM7:TR?= NVTiVYFyW0GQR1XS
U-698-M M132[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTJ7OD6yOFMh|ryP M3nFU3NCVkeHUh?=
HEL MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PSdWlEPTB;M{C5MlE1QSEQvF2= NF3Id45USU6JRWK=
KINGS-1 NGThXnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DOfWlEPTB;M{GwMlY4PCEQvF2= M1LVV3NCVkeHUh?=
KY821 M{jZS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33YdmlEPTB;M{O2MlU6PSEQvF2= MljjV2FPT0WU
MZ1-PC Mn7sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTNUFFKSzVyPUO0OU43OThizszN NXrvSnRKW0GQR1XS
LS-411N NIDLcWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHBTWM2OD1|NUSuOlYh|ryP M1nuWnNCVkeHUh?=
SIG-M5 NVLH[2hyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvyTWM2OD1|NUmuO|gzKM7:TR?= NGT6NG5USU6JRWK=
HT Mnj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXWTWM2OD1|NkeuO|EyKM7:TR?= NXvrbWxVW0GQR1XS
HC-1 NU\SOo1CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnTfolKSzVyPUO2O{44QDdizszN MoPGV2FPT0WU
NCI-H1694 MnftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\BU21KSzVyPUO3Nk46OzRizszN MU\TRW5ITVJ?
BB65-RCC MkfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;5VIZJUUN3ME2zO|YvOjR3IN88US=> M4TLTXNCVkeHUh?=
HAL-01 M3;mcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DPTGlEPTB;M{e5Mlg{QCEQvF2= MlTxV2FPT0WU
ARH-77 Mn\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTN7ND6wNFgh|ryP MmHCV2FPT0WU
MZ7-mel M3jXeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\RXo9nUUN3ME2zPVcvOjN|IN88US=> M4W1fHNCVkeHUh?=
SIMA NInwe29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LjRWlEPTB;NECzMlk{OyEQvF2= Moi4V2FPT0WU
DG-75 NUWwflBJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjK[|dKSzVyPUSxOU43QThizszN MXnTRW5ITVJ?
HUTU-80 Mle3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTRzOT6xPFUh|ryP MlvjV2FPT0WU
KNS-42 NYjwRWVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTR{NT64NVUh|ryP M136[HNCVkeHUh?=
SH-4 NIfMPYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTR{Nz61OlUh|ryP M3rYU3NCVkeHUh?=
L-540 NGTwcWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M16xeWlEPTB;NEOxMlA{OSEQvF2= M3nEWXNCVkeHUh?=
NB10 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nYRmlEPTB;NESxMlI{PCEQvF2= MVzTRW5ITVJ?
ES1 M3zPW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fQSGlEPTB;NEWyMlc2OyEQvF2= MXzTRW5ITVJ?
KMOE-2 NIfZd21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDqTI1FUUN3ME20OVYvPzFzIN88US=> MV;TRW5ITVJ?
MC116 NX7PfZlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfETWM2OD12NUiuNVE3KM7:TR?= NUXjT4FCW0GQR1XS
RCC10RGB MmrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\wTWM2OD12NkCuNFA2KM7:TR?= MYPTRW5ITVJ?
RL95-2 M3;hSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrqTWM2OD12NkCuNlM4KM7:TR?= NWjoNGFxW0GQR1XS
Raji MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\ieohKSzVyPUS2PE4yPDNizszN Mn;oV2FPT0WU
CAS-1 MmfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HSfmlEPTB;NEeyMlA4OyEQvF2= MoO2V2FPT0WU
Calu-6 M4f2Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1j3c2lEPTB;NEe1MlI3PSEQvF2= NIrkUW9USU6JRWK=
KG-1 NHzPWZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTR5OD60OEDPxE1? NGrqTHdUSU6JRWK=
LB771-HNC NF:4NW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nLc2lEPTB;NEiyMlI{OiEQvF2= NIjiTWNUSU6JRWK=
ACN M4rncGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlH4TWM2OD12OUOuOVk6KM7:TR?= MmHsV2FPT0WU
KM12 M{S1bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrKTWM2OD12OU[uOVg6KM7:TR?= NXX5OnFmW0GQR1XS

... 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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