Sonidegib (NVP-LDE225)

For research use only. Not for use in humans.

目录号：S2151 别名： Erismodegib 中文名称：索尼德吉

Sonidegib (NVP-LDE225) Chemical Structure

CAS No. 956697-53-3

Sonidegib (Erismodegib, NVP-LDE225)是一种Smoothened(Smo)拮抗剂，抑制Hedgehog (Hh)信号通路，无细胞试验中IC50分别为1.3 nM (小鼠)和2.5 nM(人)。Phase 3。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1727.35 现货
RMB 1219.02 现货
RMB 2235.15 现货
RMB 3844.77 现货
RMB 9803.43 现货
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客户使用Selleck生产的Sonidegib (NVP-LDE225)发表文献44篇：

产品安全说明书

Hedgehog/Smoothened抑制剂选择性比较

生物活性

产品描述 Sonidegib (Erismodegib, NVP-LDE225)是一种Smoothened(Smo)拮抗剂，抑制Hedgehog (Hh)信号通路，无细胞试验中IC50分别为1.3 nM (小鼠)和2.5 nM(人)。Phase 3。
特性 LDE225 是具有高效性和选择性的使平滑的拮抗剂
靶点
Smo (mouse) [1]
(Cell-free assay)		 Smo (human) [1]
(Cell-free assay)
1.3 nM 2.5 nM
体外研究

Sonidegib (Erismodegib, NVP-LDE225)可在0.6-0.8μM剂量上抑制1nM-25nM Hh激动剂Ag1.5 处理的TM3荧光报告细胞系。[1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A2780ip2 MnX4R5l1d3irY3n0fUBie3OjeR?= NU\FcmdzhjFyIN88US=> M4nXZmlEPTB;MUKg{txO M37nS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUWzN|U2Lz5{MkW1N|M2PTxxYU6=
A2780cp20 NGPS[VZEgXSxeHnjbZR6KGG|c3H5 NETpW5d,OTBizszN NVrUfFgxUUN3ME23MlUh|ryP NF30bpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW1N|M2PSd-MkK1OVM{PTV:L3G+
SKOV3ip1 MXzDfZRwgGmlaYT5JIF{e2G7 NIPVO25,OTBizszN MUHJR|UxRTJ2IN88US=> MljzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3NUOzOVUoRjJ{NUWzN|U2RC:jPh?=
SKOV3TRip2 MYXDfZRwgGmlaYT5JIF{e2G7 Mk\OglExKM7:TR?= NHzlfnhKSzVyPUGyJO69VQ>? MlixQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3NUOzOVUoRjJ{NUWzN|U2RC:jPh?=
HeyA8 M4HEWWN6fG:6aXPpeJkh[XO|YYm= M{jIUZ4yOCEQvF2= M1G4cGlEPTB;MUig{txO M2DFUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUWzN|U2Lz5{MkW1N|M2PTxxYU6=
HeyA8MDR M2j3fGN6fG:6aXPpeJkh[XO|YYm= NVHxcZkyhjFyIN88US=> MmfVTWM2OD16IN88US=> M17xb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUWzN|U2Lz5{MkW1N|M2PTxxYU6=
OS5 NXm5ZYF5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX7+OUDPxE1? NYfMRplQemWmdXPld{B1cGVicILvcIln\XKjdHnvci=> NHzkNJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K0N|U6PSd-MkOyOFM2QTV:L3G+
OS18 MmrVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mmr0glUh|ryP NULsXmNbemWmdXPld{B1cGVicILvcIln\XKjdHnvci=> M2[y[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkSzOVk2Lz5{M{K0N|U6PTxxYU6=
Glioblastoma initiating cells MlLxR5l1d3irY3n0fUBie3OjeR?= NHflUYJ,OTBizszN NXTMWolXUW6qaXLpeJMhS2WubDDWbYFjcWyrdIm= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR6Mk[3NUc,OjN2OEK2O|E9N2F-
Glioblastoma initiating cells NFrOdo9HfW6ldHnvckBie3OjeR?= NWjNWmlVhjFyIN88US=> Mo\ibY5pcWKrdIOgcoV2em:|cHjldoUh\m:{bXH0bY9v NIP2cYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S4NlY4OSd-MkO0PFI3PzF:L3G+
Glioblastoma initiating cells NWizUG5ES3m2b4jpZ4l1gSCjc4PhfS=> MmnMglExKM7:TR?= NEWyRphqdmS3Y3XzJIFxd3C2b4Ppdy=> MnXDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OEK2O|EoRjJ|NEiyOlcyRC:jPh?=
Glioblastoma initiating cells Ml7zSpVv[3Srb36gZZN{[Xl? MYD+NVAh|ryP MlPQ[I94dnKnZ4XsZZRmeyC2aHWgV2hJKHOrZ37hcIlv\yCyYYToe4F6 MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR6Mk[3NUc,OjN2OEK2O|E9N2F-
Glioblastoma initiating cells MXnGeY5kfGmxbjDhd5NigQ>? MWf+NVAh|ryP MVzJcohq[mm2czD0bIUhTXiycnXzd4lwdiCxZjDH[Y5meyCLbo\vcJZm\CCrbjDNZYlvfGGrbnnu[{BRdHW{aYDveIVv[3l? NVvofVg1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0PFI3PzFpPkKzOFgzPjdzPD;hQi=>
Glioblastoma initiating cells MV3GeY5kfGmxbjDhd5NigQ>? MlPDglExKM7:TR?= M1XSXGlvcGmkaYTzJG1wfGmuaYT5MEBKdn[jc3nvckwh[W6mIF3p[5JifGmxbh?= M1nW[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEiyOlcyLz5{M{S4NlY4OTxxYU6=
LOX IMVI NEnFUVVHfW6ldHnvckBie3OjeR?= MXuxNEDPxE1? MoqwSG1UVw>? Mnr3bY5pcWKrdIOgTIVl\2Wqb3etS2xKKHCjdHj3ZZk> MmjBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ|OUO1PVI2RC:jPh?=
UACC 257 NUG4fpFCTnWwY4Tpc44h[XO|YYm= NFHVOGgyOCEQvF2= NHzNWYdFVVOR MUnpcohq[mm2czDI[YRo\WixZz3HUGkheGG2aIfhfS=> NYPENoRRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|U6OjVpPkKzPVM2QTJ3PD;hQi=>
LOX IMVI MXvGeY5kfGmxbjDhd5NigQ>? MXyxNEDPxE1? NXKw[m84TE2VTx?= NWexe3RXcW6mdXPld{BIOSClZXzsJIN6[2ynIHHydoV{fA>? MoXBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ|OUO1PVI2RC:jPh?=
UACC 257 MVvGeY5kfGmxbjDhd5NigQ>? NHjsR40yOCEQvF2= NV;nZoVLTE2VTx?= NIfBUFdqdmS3Y3XzJGcyKGOnbHygZ5lkdGViYYLy[ZN1 NV3YNm5IRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|U6OjVpPkKzPVM2QTJ3PD;hQi=>
LOX IMVI NV\U[HdxS3m2b4jpZ4l1gSCjc4PhfS=> MmSyNVAh|ryP MWrEUXNQ Mlq4[IVkemWjc3XzJJR2dW:{IHPlcIwhfmmjYnnsbZR6 M1[y[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUO1PVI2Lz5{M{mzOVkzPTxxYU6=
UACC 257 NWLNZnVZS3m2b4jpZ4l1gSCjc4PhfS=> MlqzNVAh|ryP MlrsSG1UVw>? NXyyem1T\GWlcnXhd4V{KHS3bX;yJINmdGxidnnhZoltcXS7 MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl|NUmyOUc,OjN7M{W5NlU9N2F-
LOX IMVI NWG1c3U1SXCxcITvd4l{KGG|c3H5 Mm\lNVAh|ryP MULEUXNQ MV;pcoR2[2W|IHHwc5B1d3Orcx?= MljUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ|OUO1PVI2RC:jPh?=
UACC 257 M1\pSWFxd3C2b4Ppd{Bie3OjeR?= MmeyNVAh|ryP Mn7PSG1UVw>? MV;pcoR2[2W|IHHwc5B1d3Orcx?= MoPOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ|OUO1PVI2RC:jPh?=
ACHN M1WxOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkHrglUh|ryP MWHEUXNQ MUjJR|UxRTJvM,MAje69VQ>? MkT4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyOUO0PVEoRjJ3MEmzOFkyRC:jPh?=
769-P MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGnnfJl,PSEQvF2= MWHEUXNQ MorhTWM2OD1{LURihKnPxE1? NVLhNYd7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPVM1QTFpPkK1NFk{PDlzPD;hQi=>
786-O NHvxWGFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2jzOp42KM7:TR?= NXLOZVlwTE2VTx?= MmjVTWM2OD1{LURihKnPxE1? MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB7M{S5NUc,OjVyOUO0PVE9N2F-
786-O SuR NGT1PYNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEeyO3F,PSEQvF2= NVXad2xHTE2VTx?= NXjCfZV3UUN3ME2yMVPjiIoQvF2= M1G0NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEmzOFkyLz5{NUC5N|Q6OTxxYU6=
SP53 MWDGeY5kfGmxbjDhd5NigQ>? M3HvUFMxKM7:TR?= NFPXR5lFVVOR MV3pcohq[mm2czDj[YxtKGGmaHXzbY9vKGGwZDDtbYdz[XSrb36= NH\6Um09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki4OVYxQCd-Mk[4PFU3ODh:L3G+
SP53 M{nVSWZ2dmO2aX;uJIF{e2G7 NXjVSFVCOzBizszN NFLwU4ZFVVOR MYjpcohq[mm2czD0bIUhXkyDND3t[YRq[XSnZDDGRWshe2mpbnHsbY5oKHCjdHj3ZZk> Moi0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6OEW2NFgoRjJ4OEi1OlA5RC:jPh?=
HS5 M17yT2Z2dmO2aX;uJIF{e2G7 MYSzNEDPxE1? MYfEUXNQ NIXXXGFqdmirYnn0d{Bk\WyuIHHkbIV{cW:wIHHu[EBucWe{YYTpc44> Ml\WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6OEW2NFgoRjJ4OEi1OlA5RC:jPh?=
HS27a NGrLfHJHfW6ldHnvckBie3OjeR?= M2XhdlMxKM7:TR?= NE\6ZVlFVVOR NGT0OlRqdmirYnn0d{Bk\WyuIHHkbIV{cW:wIHHu[EBucWe{YYTpc44> MnLYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6OEW2NFgoRjJ4OEi1OlA5RC:jPh?=
SP53 M{T4fmN6fG:6aXPpeJkh[XO|YYm= NYK5VVd1OzBizszN MU\EUXNQ MWHpcoR2[2W|IHH1eI9xcGGpeR?= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh6NU[wPEc,OjZ6OEW2NFg9N2F-
Jeko MVfDfZRwgGmlaYT5JIF{e2G7 NXXjVpJpOzBizszN NYXxWJhrTE2VTx?= MUDpcoR2[2W|IHH1eI9xcGGpeR?= MknzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6OEW2NFgoRjJ4OEi1OlA5RC:jPh?=
U2OS NXPmVVZoTnWwY4Tpc44h[XO|YYm= NVPaSYlSOiCqcoO= MnixSIl{eGyjY3Xt[Y51KG:oIGuzTH1kgWOub4DhcYlv\SCocn;tJJdqdGRidInw[UBUdW9iZYjwdoV{e2WmIHnuJHUzV1NiY3XscJMh[W[2ZYKgNkBpenNiYomgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiS3mgQUAxNjByNjFOwG0v MkT5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyNkO1NlIoRjJ|ME[zOVIzRC:jPh?=
NIH/3T3 NIe4PIdHfW6ldHnvckBie3OjeR?= Mo\RTY5pcWKrdHnvckBw\iCqZXTn[Yhw\yC|aXfuZYxqdmdicHH0bJdigSCrbjDtc5V{\SCQSVivN3Q{KGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKFOvbzDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iR3zpJI1TVkFiZYjwdoV{e2mxbjDifUBTXC2SQ2KgcYV1cG:mLDDJR|UxKD1iMD6wNFQ1KM7:TT6= MlXWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd6MUC1PVEoRjJ5OEGwOVkyRC:jPh?=
NIH/3T3 MUDGeY5kfGmxbjDhd5NigQ>? MYDJcohq[mm2aX;uJI9nKGinZHflbI9oKHOrZ37hcIlv\yCyYYToe4F6KGmwIH3veZNmKE6LSD:zWFMh[2WubIOgbIFz[m:{aX7nJHNudyCGNEe3TEBufXSjboSgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIFfsbUBuWk6DIHX4dJJme3Orb36gZpkhWlRvUFPSJI1mfGixZDygTWM2OCB;IECuNFIzPyEQvF2u MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzhzMEW5NUc,Ojd6MUC1PVE9N2F-
NIH/3T3 NG[xO49HfW6ldHnvckBie3OjeR?= MnyxNlQhcHK| Ml3DTY5pcWKrdHnvckBw\iCqZXTn[Yhw\yC|aXfuZYxqdmdicHH0bJdigSCrbjDtc5V{\SCQSVivN3Q{KGOnbHzzJI1m[XO3cnXkJIFnfGW{IEK0JIhzeyCkeTDHcIku\HWjbDDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUCgQUAxNjByNjFOwG0v MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzhzMEW5NUc,Ojd6MUC1PVE9N2F-
TM3 M4G1RmZ2dmO2aX;uJIF{e2G7 MlfUOFghcHK| NH;yemZKdmirYnn0bY9vKG:oIFjoJJNq\26jbHnu[{Bx[XSqd3H5JIlvKG2xdYPlJHROOyClZXzsd{Bie3Onc4Pl[EBieyCmb4fudoVofWyjdHnvckBw\iCJbHmxJIdmdmViZYjwdoV{e2mxbjDh[pRmeiB2ODDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyIE2gNE4xODF{IN88UU4> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl5NkKxOUc,OjZ7N{[yNVU9N2F-
NIH3T3 MWDGeY5kfGmxbjDhd5NigQ>? M4DPSFQ5KGi{cx?= NIH2eIJKdmirYnn0bY9vKG:oIGPITEB{cWewYXzpcocheGG2aIfhfUBqdiCvb4Xz[UBPUUh|VEOgZ4VtdHNibXXhd5Vz\WRiYX\0[ZIhPDhiaILzJIJ6KEeuaT3seYNq\mW{YYPlJJJmeG:{dHXyJIF{e2G7LDDJR|UxKD1iMD6wNFU2KM7:TT6= Mmm5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzN{[zPVYoRjJ2MUe2N|k3RC:jPh?=
NIH3T3 NWe0T5lkTnWwY4Tpc44h[XO|YYm= NIfyU|I1QCCqcoO= M4LDemlvcGmkaYTpc44hd2ZiU3;ubYMucW6mdXPl[EBp\WSpZXjv[{B{cWewYXzsbY5oKGmwIH3veZNmKE6LSEPUN{Bk\WyuczDh[pRmeiB2ODDodpMh[nliR3zpMYx2[2moZYLhd4UhemWyb4L0[ZIh[XO|YYmsJGlEPTBiPTCwMlAxPTVizszNMi=> M2npbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OEKwOVU1Lz5{NkiyNFU2PDxxYU6=
NIH/3T3 MWrGeY5kfGmxbjDhd5NigQ>? MXzJcohq[mm2aX;uJI9nKGinZHflbI9oKHOrZ37hcIlv\yCyYYToe4F6KGW6cILld5Nm\CCrbjDtc5V{\SCQSVivN3Q{KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gbIVl\2Wqb3etbY5lfWOnZDDHcIkuOiCjY3P1cZVt[XSrb36gZZQhfGmyIH;mJJBzcW2jcomgZ4ltcWFiYomgSGFRUSC|dHHpcolv\yCkYYPl[EBkd26ob3PhcEBucWO{b4Pjc5Bq[yCjbnHsfZNqew>? MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzhzMEW5NUc,Ojd6MUC1PVE9N2F-
NIH/3T3 NUHWeGVUTnWwY4Tpc44h[XO|YYm= M{\X[GlvcGmkaYTpc44hd2ZiaHXk[4Vpd2dic3nncoFtcW6pIIDheIh4[XliaX6gcY92e2ViTlnIM|NVOyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJIhm\GenaH;nMYlv\HWlZXSgV41wNUWJRmCgZ4ltcWG{eTD0doFve2yxY3H0bY9vKGK7IFTBVGkhe3SjaX7pcoch[mG|ZXSgZ49v\m:lYXygcYlkem:|Y3;wbYMh[W6jbInzbZM> Mkj0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd6MUC1PVEoRjJ5OEGwOVkyRC:jPh?=
MG 63 (6-TG R) NIX5VZhyUFSVIHHzd4F6 NVry[W9EeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? M4mxNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41 NUHlfXRCeUiWUzDhd5NigQ>? M1nzUJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpPDFiY3XscJM> M2rXZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
U-2 OS MnTEdWhVWyCjc4PhfS=> MnjYdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWU0zKE:VIHPlcIx{ NXzTO2RWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673 MWrxTHRUKGG|c3H5 NG\wN2tyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= NGDXe3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-12 MWXxTHRUKGG|c3H5 NVLCN3BZeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVEzKGOnbHzz Mk[5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R) NHvlT3lyUFSVIHHzd4F6 NWS4fIFxeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz NY[xOHp1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB-EBc1 MoDHdWhVWyCjc4PhfS=> MULxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 MoPSdWhVWyCjc4PhfS=> NX2xRlV2eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Saos-2 MkfjdWhVWyCjc4PhfS=> MVrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| M3;uS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2 MmnFdWhVWyCjc4PhfS=> MW\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC NHLDOWVyUFSVIHHzd4F6 MlHzdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= MkfNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-SH M3vsfpFJXFNiYYPzZZk> NWPQfFlDeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM> M4rUb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
Bcl2 / c-myc / Cyclin D1 / pERK / ERK / pJNK / JNK / Caspase 3 / Cleaved caspase 3 ; 

PubMed: 22821765     


Immunoblot experiment of protein lysate from OPM1 cells treated with NVP-LDE225 (5μM) for 12, 24, and 36 hours and fractionated by electrophoresis and stained with different Abs as shown in figure (left). Cells were treated with different concentrations o䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෕Ð鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸

Gli-1 / Gli-2 / p-Akt / Akt; 

PubMed: 25093491     


Western blot analysis on total cell lysates from renal cancer cell lines treated with NVP-LDE225 at different concentrations. Densitometric measurements were normalised to β-actin and reported under western blot images.

pp70S6K / P70s6k; 

PubMed: 25093491     


Percentage of survival of 786-O, 786-O SuR, and 769-P renal cancer cell lines treated with NVP-LDE225 and everolimus or their combination, as measured by the MTT assay. Data represent the mean (±s.d.) of three independent experiments, each performed in tr䲧疝Ỵ疞㧀疜膉痘 瘿뙠ෆᾰƌෆĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ෆĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ�෋䐺痖暼瘿�෋ᾰƌ �෋Ð㺣痖�෋€𢡄�෋€䀷痗�෋౴�෋㵶痗�෋뺖᎒泌Itemｾ᎒Count﫨呂�෋猴፲�

p-p130CAS / p130CAS / p-FAK / FAK / p-Paxillin / Paxillin; 

PubMed: 25093491     


Western blot analysis of total cell lysates from 786-O, 786-O SuR, and 769-P human renal cancer cell lines treated with NVP-LDE225 (2.5 μm), everolimus (1 μm), and their combination. Densitometric measurements were normalised to β-actin and reported under䲧疝Ỵ疞㧀疜膉痘 

22821765 25093491
Immunofluorescence
GLI1; 

PubMed: 22821765     


U266 were cultured in the presence of control medium or NVP-LDE225 (5μM) for 24 hours. Immunocytochemical analysis was assessed using anti-Gli1 Ab, and 4,6-diamidino-2-phenylindole was used to stain nuclei. The cells were analyzed using an epifluorescence䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෕Ð鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ뙠ෆ䐺痖暼瘿뙠ෆᾰƌ 뙠ෆÐ㺣痖뙠ෆ€𢡄뙤ෆ€

22821765
体内研究 Sonidegib (Erismodegib, NVP-LDE225)与小鼠，大鼠以及人源的血浆蛋白有很强的结合能力(>99%)，同时与狗和猴子的血浆蛋白有适度的结合，结合能力分别是77 %和 85%。PAMPA 实验证明LDE225能够达到90.8%的渗透性。在梯度稀释的试验中，LDE225在临床物种上显示出很好的口服药效率，其生物药效率在69%到102%之间。LDE225呈弱碱性，pKa只有4.20，同时它的水溶性也相对较弱。LDE225被证明具有剂量依赖的抗肿瘤活性。给药剂量在5 mg/kg/天，一天一次时，LDE225明显抑制肿瘤生长，与33%的T/C值相一致。给药剂量在10 mg/kg/天，一天一次和 20 mg/kg/天，一天一次时，LDE225促使肿瘤退化的效果分别达到51%和83%。Gli1 mRNA抑制性与LDE225介导的肿瘤与血浆接触有关。在肿瘤移植的动物模型中，经过四天的给药处理，LDE225能够成功地穿过血脑屏障导致肿瘤生长受抑制[1]。LDE225能够使Rip1-Tag2小鼠中的肿瘤体积明显减少95.7%。LDE225减少LDE225给药处理小鼠的间质状标志基因的表达[2]。

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验：

[1]
- 合并
  • Cell lines: TM3Hh12 细胞
  • Concentrations: 0 μM -10 μM
  • Incubation Time: 30 分钟
  • Method:

    LDE225 用DMSO连续稀释后加入空的分析平板中。TM3Hh12 细胞 (TM3 细胞含有Hh的应答报告基因元件pTA-8xGli-Luc) 用含有5%的马血清，2.5%的胎牛血清(FBS)和15 mM HEPES, pH 7.3的F12 Ham’s/DMEM (1:1)培养基培养。收集细胞时用胰酶消化，然后用含有5%的马血清和15 mM HEPES, pH 7.3的F12 Ham’s/DMEM (1:1)培养基重悬，接着分铺到分析板中。然后加入LDE225在37 °C ，5% CO2的培养箱中大约孵育30分钟。接着加入1 nM 和25 nM 的Ag1.5到分析平板中，37 °C ，5% CO2的条件下培养。48小时后，向平板中加入Bright-Glo 或者 MTS试剂，测量492纳米下的荧光值或者吸收峰。通过MTS法检测Gli-驱动荧光素酶发光或吸光度信号，对浓度取Log（10）值做由非线性回归曲线，确定IC 50值。数据处理使用R统计软件包。


    (Only for Reference)
动物实验：

[1]
- 合并
  • Animal Models: 采用无胸腺裸小鼠建立原位Ptch+/-p53-/-髓母细胞瘤同种异体移植模型
  • Dosages: 40 mg/kg/天
  • Administration: 口服，每天两次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 97 mg/mL (199.79 mM)
Ethanol 97 mg/mL warmed (199.79 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)：
2% DMSO+corn oil
 10mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 485.5
化学式

C26H26F3N3O3
CAS号 956697-53-3
储存条件 粉状
溶于溶剂
别名 Erismodegib

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量 只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量：

总分子量：g/mol

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02358161 Completed Drug: gemcitabine and nab paclitaxel Pancreatic Cancer Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)|Novartis|Celgene Corporation September 2015 Phase 1|Phase 2
NCT02254551 Terminated Drug: LDE225|Drug: Bortezomib Multiple Myeloma SCRI Development Innovations LLC|Novartis January 2015 Phase 2
NCT02138929 Completed Drug: Everolimus|Drug: LDE 225 Esophageal Cancer M.D. Anderson Cancer Center|Novartis|National Cancer Institute (NCI) November 10 2014 Phase 1
NCT02195973 Completed Drug: LDE225 Recurrent Ovarian Cancer University of Alabama at Birmingham|Novartis Pharmaceuticals September 2014 Phase 1
NCT02027376 Completed Drug: LDE225|Drug: Docetaxel Advanced Breast Cancer Spanish Breast Cancer Research Group|Novartis May 2014 Phase 1
NCT02111187 Completed Drug: LDE225 Prostate Cancer Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins April 2014 Phase 1

技术支持

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操作手册

如果有其他问题，请给我们留言。

  • * 必填项
Selleck产品目录册

Hedgehog/Smoothened Signaling Pathway Map

Hedgehog/Smoothened Inhibitors with Unique Features

  • 选择性强的Smoothened抑制剂

    PF-5274857 : Smoothened-selective, IC50=5.8 nM.

  • 用于临床的Smoothened抑制剂

    LDE225 (NVP-LDE225,Erismodegib) : Phase III for Hh-pathway activated relapsed Medulloblastoma (MB).

  • 最新的Smoothened抑制剂

    GANT61 : 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.

  • Smoothened激活剂

    Purmorphamine : Directly binds and activates Smoothened, and blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM.

相关Hedgehog/Smoothened产品

  • Smoothened Agonist (SAG) HCl New

    Smoothened Agonist (SAG) HCl是一种细胞渗透性Smoothened (Smo)激动剂，其在Shh-LIGHT2细胞中的EC50约为3 nM。

  • SB225002 New

    SB225002是一种强效的选择性CXCR2拮抗剂，抑制白介素IL-8与CXCR2的结合，IC50为22 nM，选择性比其它测试的7-TMRs高150多倍。

  • SB-334867 New

    SB-334867 是一种选择性 orexin-1 (OX1) receptor 拮抗剂。

  • Vismodegib (GDC-0449)

    Vismodegib (GDC-0449)是一种新型有效的，特异性hedgehog抑制剂，无细胞试验中IC50为3 nM，也会抑制P-gp，IC50为3.0μM。

  • Cyclopamine

    Cyclopamine (11-deoxojervine)是一种特异性Hedgehog (Hh)信号通路拮抗剂，作用于Smoothened (Smo)，在TM3Hh12细胞中IC50为46 nM。

  • GANT61

    GANT61 (NSC 136476)是一种GLI1及GLI2诱导的转录抑制剂，抑制hedgehog，在表达GLI1的HEK293T细胞中IC50为5 μM，选择性作用于其他通路，如TNF和糖皮质激素受体基因的转录。GANT61在LX-2细胞中可诱导凋亡并激活保护性自噬。

  • Purmorphamine

    Purmorphamine (Shh Signaling Antagonist VI)直接结合并激活Smoothened，阻断BODIPY-cyclopamine与Smo结合，在HEK293T细胞中IC50约为1.5 μM，也诱导成骨细胞分化，EC50为1μM。Purmorphamine 可减少基础和诱导的自噬。

  • Taladegib (LY2940680)

    Taladegib (LY2940680)与Smoothened(Smo)受体结合，有效抑制Hedgehog(Hh)信号通路。Phase 1/2。

  • Glasdegib (PF-04449913)

    Glasdegib（PF-04449913）是一种强效且口服生物有效的Smoothened (Smo)抑制剂，其IC50为5 nM。Phase 2。

  • SANT-1

    SANT-1直接结合到Smoothened (Smo)受体，Kd为1.2 nM，且抑制smo激动剂作用效果，IC50为20 nM。

    Features:SANT-1比其他拮抗剂更大程度地降低SAG对Shh-LIGHT2细胞的刺激。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID