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)

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 Moq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTVwOE[2OkDPxE1? MUjTRW5ITVJ?
DOHH-2 Mn;ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fXeGlEPTB;OT6zOVY5QSEQvF2= MkS1V2FPT0WU
no-10 MmH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7aTWM2OD17LkmwN|kh|ryP NIX1c4RUSU6JRWK=
LS-513 NUjCRVBwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTjPGhKSzVyPUGxMlM2PDdizszN NYPiOWJZW0GQR1XS
ALL-PO MmLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XiXmlEPTB;MUGuO|c{PCEQvF2= MULTRW5ITVJ?
8-MG-BA NEDMUWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7uTWM2OD1zMz6xNVI{KM7:TR?= NEDlT5dUSU6JRWK=
RPMI-8402 MofhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fabWlEPTB;MUWuPFU{PyEQvF2= NH74b5ZUSU6JRWK=
EoL-1-cell NWfqRZZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7jUWZvUUN3ME2xPE42QTR6IN88US=> NYLxOYhNW0GQR1XS
NALM-6 NVXtNXZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PQT2lEPTB;MUmuNFE3PyEQvF2= NIC3PY9USU6JRWK=
DEL MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLNSGFKSzVyPUKwMlE1PzFizszN NHzmVXlUSU6JRWK=
SR NYLGNohpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVv0WWtwUUN3ME2yN{43PzF3IN88US=> MXnTRW5ITVJ?
697 Mn7vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGThS25KSzVyPUK2MlYyPTVizszN MkHFV2FPT0WU
COLO-829 M1;1fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTBTWM2OD1{Nj64OFg{KM7:TR?= MVXTRW5ITVJ?
EVSA-T M3TwOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXhXFdXUUN3ME2yO{42PTZzIN88US=> NUi5bmVbW0GQR1XS
ATN-1 NHnOXXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HYSWlEPTB;M{GuNlMzQSEQvF2= M{[zOXNCVkeHUh?=
L-363 NGGzR5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nGVGlEPTB;M{GuO|Q3OSEQvF2= MmfaV2FPT0WU
LAMA-84 M2HEW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV24NYpuUUN3ME2zNk42OjFzIN88US=> Mnv2V2FPT0WU
NOS-1 NEHoSIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HNe2lEPTB;M{SuNlk2PiEQvF2= NUXKPJY6W0GQR1XS
BB30-HNC MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLXTWM2OD1|ND6zN|A3KM7:TR?= MoLqV2FPT0WU
BC-1 MmDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkniTWM2OD1|Nz65O|Q3KM7:TR?= MknkV2FPT0WU
IST-SL2 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPaWZo2UUN3ME2zPE4zOjRizszN MlfxV2FPT0WU
D-392MG NVjo[|B5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jJTmlEPTB;NECuNlIyPSEQvF2= NIXKZnNUSU6JRWK=
no-11 NVvTT5hzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fafWlEPTB;NECuOVUzOSEQvF2= NXrTcJFjW0GQR1XS
LC4-1 NWjYPG01T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;EUlhKSzVyPUSwMlg4OTZizszN NIfGTZRUSU6JRWK=
A388 NEjDSlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDVflRKSzVyPUSyMlU5PDhizszN NYfwOXhnW0GQR1XS
NTERA-S-cl-D1 M13UUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TVbmlEPTB;NEKuO|A4PCEQvF2= M3rjfnNCVkeHUh?=
CESS NVjOXmxVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\YTGlEPTB;NESuNlI{OiEQvF2= M3;uNnNCVkeHUh?=
RS4-11 M3Lpdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fWVWlEPTB;NEmuNFk{QCEQvF2= MXfTRW5ITVJ?
MS-1 NU\WU5pYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnOcoI5UUN3ME21NE46OzVzIN88US=> NE[xcFlUSU6JRWK=
CTV-1 NW\FPId5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HvbGlEPTB;NUGuNFc1KM7:TR?= M3\ROXNCVkeHUh?=
D-502MG M33QR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\2TWM2OD13MT62NlcyKM7:TR?= NFL5fHNUSU6JRWK=
ML-2 NWOwcHZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILjU5VKSzVyPUWyMlkyQTVizszN NHzTZ5BUSU6JRWK=
SK-NEP-1 NGrHfphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nad2lEPTB;NUOuN|kzOyEQvF2= MXfTRW5ITVJ?
LOXIMVI MmHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4WxdGlEPTB;NUOuOVg5PCEQvF2= M2D1OnNCVkeHUh?=
DJM-1 NYPFW3l4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTV4LkOzPVEh|ryP NX\i[3RIW0GQR1XS
GI-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXvOFNuUUN3ME21Ok43OTR7IN88US=> MYHTRW5ITVJ?
IST-MES1 NEDye21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTZyLkW0PVMh|ryP NUjJWnE{W0GQR1XS
MV-4-11 NFGxR2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fRTGlEPTB;NkCuOlU{QCEQvF2= M33EOnNCVkeHUh?=
OVCAR-4 M4TpOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIKzcpFKSzVyPU[zMlU3PTdizszN MkLZV2FPT0WU
KE-37 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlGzTWM2OD14Nj6yOlY5KM7:TR?= NI[5fZlUSU6JRWK=
D-542MG M33Ge2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XGOWlEPTB;NkiuOFE{PSEQvF2= NFvwN4tUSU6JRWK=
MHH-PREB-1 MnLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTd{Lki0OFEh|ryP NHLTdGhUSU6JRWK=
MRK-nu-1 MlvLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzyTWM2OD15Mz60O|A2KM7:TR?= NH\CZ3hUSU6JRWK=
D-247MG NXnp[WY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmmwTWM2OD15Mz61OFQzKM7:TR?= M1vsV3NCVkeHUh?=
OCI-AML2 NXq1NmlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3pTWM2OD15Nj65N|Y6KM7:TR?= MXfTRW5ITVJ?
LP-1 NY[zfWRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnLTWM2OD16Mj64O|MyKM7:TR?= MUjTRW5ITVJ?
HCC1599 M37GNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;mdmlEPTB;OESuNlg{PyEQvF2= NHnBb|BUSU6JRWK=
KARPAS-45 MlHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDBTWM2OD16ND62PVkzKM7:TR?= NFq4dnFUSU6JRWK=
BE-13 NF\KTppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUWyT5JyUUN3ME25PU4xPDd5IN88US=> NIfNRXlUSU6JRWK=
GCIY MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\vTWM2OD17OT6wPVU1KM7:TR?= M{jYPXNCVkeHUh?=
BV-173 M3y1fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLNVmtKSzVyPUGwNE4{OjVizszN NX70[GZOW0GQR1XS
LB2518-MEL M3Kzfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTFyMD63PFkh|ryP MWjTRW5ITVJ?
KS-1 MkLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTFyMT62N|kh|ryP NYfF[VBRW0GQR1XS
MOLT-16 NGTW[IlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1P2b2lEPTB;MUC0Mlk5PiEQvF2= NWK3XmlyW0GQR1XS
NCI-H1770 NGXp[|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnOeYhZUUN3ME2xNFgvPzh2IN88US=> NEPYTJdUSU6JRWK=
NCI-H82 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLTdFMxUUN3ME2xNVAvQTd4IN88US=> M2\ycXNCVkeHUh?=
NCCIT M2rkRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfmR4VKSzVyPUGxNk42OjlizszN NYL5SFlkW0GQR1XS
KALS-1 MlrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDXTWM2OD1zMUWuPVQyKM7:TR?= M4TuU3NCVkeHUh?=
LB2241-RCC NV[yfY5{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M172[2lEPTB;MUG2MlY4QSEQvF2= NI[4NWpUSU6JRWK=
HH NGfhPXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITISJNKSzVyPUGxO{4{QTVizszN MlXBV2FPT0WU
HD-MY-Z NHy0SldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUf5U4kyUUN3ME2xNVgvPDh6IN88US=> Mne4V2FPT0WU
EB-3 M3;mc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEX4U3BKSzVyPUGyN{4xQTRizszN NWS0ZW17W0GQR1XS
BL-70 M3TWN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTF{Mz6xNlch|ryP NX;JVINzW0GQR1XS
K-562 NUj1XZo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\YVW9EUUN3ME2xNlYvOjR3IN88US=> NX7ySW5zW0GQR1XS
HT-144 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTF|Mz6xOlQh|ryP NFmydlNUSU6JRWK=
PF-382 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jsdmlEPTB;MUO0MlM3OSEQvF2= NH35WlFUSU6JRWK=
RPMI-8226 NWjZZ5VTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rie2lEPTB;MUO1MlA1PSEQvF2= MV3TRW5ITVJ?
NCI-H1355 M2\YNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTF|NT61PFch|ryP MVjTRW5ITVJ?
LXF-289 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonaTWM2OD1zM{muO|gyKM7:TR?= NEW1XZdUSU6JRWK=
NCI-H69 MlfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnW4TWM2OD1zNEKuPVMzKM7:TR?= M3;xbXNCVkeHUh?=
SK-MEL-1 NGfWfJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWX4UXpMUUN3ME2xOFcvOTNizszN NH74R4ZUSU6JRWK=
KARPAS-299 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTF2OT6xNkDPxE1? MoLRV2FPT0WU
GB-1 MlPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7NWo1KSzVyPUG0PU4{OjJizszN MmPwV2FPT0WU
CMK NXn4TXZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXvNopxUUN3ME2xOFkvPTF3IN88US=> NETiRpNUSU6JRWK=
MPP-89 NXnFTHBsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTF3Nj6wN|Uh|ryP NEL5eFJUSU6JRWK=
KU812 NYHmb|VPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXMeHBKSzVyPUG2NU46ODJizszN NWjhRmZvW0GQR1XS
REH NEToNYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\EXXZ[UUN3ME2xOlIvOTJ3IN88US=> MmDhV2FPT0WU
NEC8 NIXU[I5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljaTWM2OD1zNkWuNFI3KM7:TR?= NGq4NYxUSU6JRWK=
KP-N-YS NGfPT5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjUTJVWUUN3ME2xOlgvOzl3IN88US=> MlXTV2FPT0WU
Ramos-2G6-4C10 M3rxWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vv[mlEPTB;MU[5MlkyPSEQvF2= M13zeHNCVkeHUh?=
Becker M2LvSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HLS2lEPTB;MUe0MlE5KM7:TR?= M1fPZ3NCVkeHUh?=
LB647-SCLC M2PQXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnFTWM2OD1zN{WuPFQ2KM7:TR?= NYrjcI9UW0GQR1XS
LU-139 MkHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDJVY9KSzVyPUG3PE4xOTlizszN MlfOV2FPT0WU
QIMR-WIL MlXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\kd5R[UUN3ME2xO|kvPjR4IN88US=> M{n1SnNCVkeHUh?=
NCI-H1395 NHHMb|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPJS2FnUUN3ME2xO|kvQTl4IN88US=> M4Lyc3NCVkeHUh?=
NOMO-1 MnjXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XtWWlEPTB;MUiyMlg2KM7:TR?= NHHpZ3BUSU6JRWK=
GI-ME-N MoP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTzV2xKSzVyPUG4O{46PjlizszN MU\TRW5ITVJ?
KMS-12-PE NVm2c2s3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\uTWM2OD1zOEmuNlc{KM7:TR?= NXXI[nBoW0GQR1XS
Daudi MmDmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX2wWYN2UUN3ME2xPVEvOTJ6IN88US=> MVTTRW5ITVJ?
LB996-RCC NH7zSoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTF7MT62PVkh|ryP MmjVV2FPT0WU
NCI-H2107 NVqwdXdDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3aTWM2OD1zOUOuO|M6KM7:TR?= NVPlWIpPW0GQR1XS
SK-PN-DW Mle4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;MTWM2OD1zOUSuO|E6KM7:TR?= NVzqVYxjW0GQR1XS
MC-CAR NVHqdIl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmC0TWM2OD1{MEKuNlU{KM7:TR?= NWjTVYNoW0GQR1XS
SNB75 NH;yU5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETiVoNKSzVyPUKyNU46PCEQvF2= MoT4V2FPT0WU
ES4 MlflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nOW2lEPTB;MkKzMlc5OyEQvF2= MkTtV2FPT0WU
KARPAS-422 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnlSJMyUUN3ME2yNlgvOzV{IN88US=> NUPWUYlGW0GQR1XS
NCI-H1648 M4DqPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\5TWM2OD1{MkmuOFg6KM7:TR?= NU\TN4FpW0GQR1XS
ES6 NWWzNmVoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fFSGlEPTB;MkO5MlQ{KM7:TR?= NEDnU4FUSU6JRWK=
KNS-81-FD MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEi5VYlKSzVyPUK0NU4yQTdizszN M1zuSHNCVkeHUh?=
JAR M4\ufmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTJ3Nj6yNlUh|ryP MVfTRW5ITVJ?
NB1 NIrkSFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvUZYtKSzVyPUK2NE42OTZizszN NYHVVlN1W0GQR1XS
D-336MG M2KyVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXPUoRmUUN3ME2yOlAvPjl6IN88US=> M4jYTnNCVkeHUh?=
BC-3 M1T5RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7sZldKSzVyPUK2OU4yPzhizszN MlfVV2FPT0WU
HCC2218 MkDRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nBc2lEPTB;Mk[2MlQyPSEQvF2= NHXk[FZUSU6JRWK=
TE-9 MkL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTJ4Nj62Nlch|ryP NUS3T|JtW0GQR1XS
LB1047-RCC NYjOepVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3Tkb2lEPTB;Mk[2Mlc2OyEQvF2= NHm1Wm9USU6JRWK=
CTB-1 Mn7MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HZOmlEPTB;Mk[5Mlk4OyEQvF2= MnfhV2FPT0WU
NB7 M3H4Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vSOWlEPTB;MkexJO69VQ>? MkjuV2FPT0WU
ST486 NGXhO3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fqfmlEPTB;Mke3MlQyOiEQvF2= NV\sVplYW0GQR1XS
HCC1187 NFPJVYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXNOJlKSzVyPUK4Nk45OTFizszN MnK4V2FPT0WU
NCI-SNU-16 NFXle3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXziXII4UUN3ME2yPFQvOjR6IN88US=> NWDyVZF7W0GQR1XS
COR-L279 MlXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDlTWM2OD1{OUGuOVg1KM7:TR?= M{fTPHNCVkeHUh?=
ES8 NYfReGZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTJ7ND6xPFIh|ryP NVTPTWJzW0GQR1XS
U-698-M NYKycINjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mly0TWM2OD1{OUiuNlQ{KM7:TR?= MVjTRW5ITVJ?
HEL M1O0Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTNyOT6xOFkh|ryP M{\zeHNCVkeHUh?=
KINGS-1 M2TkdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfXcYFKSzVyPUOxNE43PzRizszN NXfoSplXW0GQR1XS
KY821 NYPYdpdwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXBS5BKSzVyPUOzOk42QTVizszN M3zWT3NCVkeHUh?=
MZ1-PC MnzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVywT2g2UUN3ME2zOFUvPjF6IN88US=> MYDTRW5ITVJ?
LS-411N MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmT3TWM2OD1|NUSuOlYh|ryP MUnTRW5ITVJ?
SIG-M5 NEHGOVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTN3OT63PFIh|ryP NVPWSmhJW0GQR1XS
HT NIS4XZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDLNItiUUN3ME2zOlcvPzFzIN88US=> MorSV2FPT0WU
HC-1 MlLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTN4Nz63PFch|ryP NGPRbZFUSU6JRWK=
NCI-H1694 NXzIV5BET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTN5Mj65N|Qh|ryP NXfCN5NIW0GQR1XS
BB65-RCC MoS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTvTWM2OD1|N{[uNlQ2KM7:TR?= NXTOWG9XW0GQR1XS
HAL-01 NFq5S2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTN5OT64N|gh|ryP MYjTRW5ITVJ?
ARH-77 NWm5OHJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moq1TWM2OD1|OUSuNFA5KM7:TR?= M{nOdnNCVkeHUh?=
MZ7-mel MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXRTWM2OD1|OUeuNlM{KM7:TR?= MUDTRW5ITVJ?
SIMA MkLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFT6Z2xKSzVyPUSwN{46OzNizszN NF\TR25USU6JRWK=
DG-75 NGjHXmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2D6XGlEPTB;NEG1MlY6QCEQvF2= MXjTRW5ITVJ?
HUTU-80 MoDUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH:yZo9KSzVyPUSxPU4yQDVizszN NELkXG9USU6JRWK=
KNS-42 MlG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XjcGlEPTB;NEK1MlgyPSEQvF2= NVe4OnY4W0GQR1XS
SH-4 M1;tVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTR{Nz61OlUh|ryP NUnrXJp7W0GQR1XS
L-540 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnL[nlKSzVyPUSzNU4xOzFizszN NXG3SplHW0GQR1XS
NB10 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHhTWM2OD12NEGuNlM1KM7:TR?= MWHTRW5ITVJ?
ES1 NFSzfplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTR3Mj63OVMh|ryP MmCzV2FPT0WU
KMOE-2 MnPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrjVZBKSzVyPUS1Ok44OTFizszN MXLTRW5ITVJ?
MC116 NWTWT3ByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHT2S|FKSzVyPUS1PE4yOTZizszN NEKxfZNUSU6JRWK=
RCC10RGB M1fVfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWiydnRnUUN3ME20OlAvODB3IN88US=> MoHvV2FPT0WU
RL95-2 Mmq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXGTnhQUUN3ME20OlAvOjN5IN88US=> NIXLd3hUSU6JRWK=
Raji M{P5Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV20RphNUUN3ME20OlgvOTR|IN88US=> M2SybXNCVkeHUh?=
CAS-1 MofmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXufFZKSzVyPUS3Nk4xPzNizszN MkjTV2FPT0WU
Calu-6 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LxWmlEPTB;NEe1MlI3PSEQvF2= MUDTRW5ITVJ?
KG-1 M361VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjWNHNKSzVyPUS3PE41PCEQvF2= NIr1cmNUSU6JRWK=
LB771-HNC NHzPcmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\SSGlEPTB;NEiyMlI{OiEQvF2= M2HvOXNCVkeHUh?=
ACN Mn:2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TyV2lEPTB;NEmzMlU6QSEQvF2= NFS3S4hUSU6JRWK=
KM12 MnrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;jOmlEPTB;NEm2MlU5QSEQvF2= M2[2VXNCVkeHUh?=

... 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 (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 is a cell-permeable Smoothened (Smo) agonist.

  • 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