Sonidegib (NVP-LDE225)

目录号:S2151 别名: Erismodegib 中文名称:索尼德吉

仅限科研使用

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。

Sonidegib (NVP-LDE225) Chemical Structure

CAS: 956697-53-3

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 3844.77 现货
RMB 9803.43 现货
大包装 有超大折扣
大剂量询单有大折扣!

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Sonidegib (NVP-LDE225)发表文献52篇:

产品安全说明书

Hedgehog/Smoothened抑制剂选择性比较

相关Hedgehog/Smoothened产品

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 MlXBR5l1d3irY3n0fUBie3OjeR?= NW[2OZdphjFyIN88US=> MXTJR|UxRTF{IN88US=> NV\neoxxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1OVM{PTVpPkKyOVU{OzV3PD;hQi=>
A2780cp20 MUjDfZRwgGmlaYT5JIF{e2G7 MofhglExKM7:TR?= NFnrdmdKSzVyPUeuOUDPxE1? NFjuR5g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW1N|M2PSd-MkK1OVM{PTV:L3G+
SKOV3ip1 M{X2[WN6fG:6aXPpeJkh[XO|YYm= MYT+NVAh|ryP MVrJR|UxRTJ2IN88US=> NHroNJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW1N|M2PSd-MkK1OVM{PTV:L3G+
SKOV3TRip2 M1vLXmN6fG:6aXPpeJkh[XO|YYm= Mne2glExKM7:TR?= MlzyTWM2OD1zMjFOwG0> NY\MTnRsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1OVM{PTVpPkKyOVU{OzV3PD;hQi=>
HeyA8 MoXzR5l1d3irY3n0fUBie3OjeR?= MUX+NVAh|ryP MnjOTWM2OD1zODFOwG0> MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV3M{O1OUc,OjJ3NUOzOVU9N2F-
HeyA8MDR MYrDfZRwgGmlaYT5JIF{e2G7 Mor2glExKM7:TR?= M4TG[WlEPTB;ODFOwG0> NE\FfpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW1N|M2PSd-MkK1OVM{PTV:L3G+
OS5 M3rEUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYTuTplLhjVizszN MmHZdoVlfWOnczD0bIUheHKxbHnm[ZJifGmxbh?= MnfXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{NEO1PVUoRjJ|MkSzOVk2RC:jPh?=
OS18 MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXm2SoM2hjVizszN MX7y[YR2[2W|IITo[UBxem:uaX\ldoF1cW:w MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ2M{W5OUc,OjN{NEO1PVU9N2F-
Glioblastoma initiating cells NGfHSWtEgXSxeHnjbZR6KGG|c3H5 MV;+NVAh|ryP M3nrcmlvcGmkaYTzJGNmdGxiVnnhZoltcXS7 M3i5RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEiyOlcyLz5{M{S4NlY4OTxxYU6=
Glioblastoma initiating cells M33XRWZ2dmO2aX;uJIF{e2G7 NGfaZ2J,OTBizszN NGrTdWlqdmirYnn0d{Bv\XW{b4PwbIVz\SCob4LtZZRqd25? MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR6Mk[3NUc,OjN2OEK2O|E9N2F-
Glioblastoma initiating cells MoPGR5l1d3irY3n0fUBie3OjeR?= M1PYOJ4yOCEQvF2= NILNZVVqdmS3Y3XzJIFxd3C2b4Ppdy=> M4T6XFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEiyOlcyLz5{M{S4NlY4OTxxYU6=
Glioblastoma initiating cells M3LJVmZ2dmO2aX;uJIF{e2G7 M4SxWp4yOCEQvF2= NHjnSYxld3ewcnXneYxifGW|IITo[UBUUEhic3nncoFtcW6pIIDheIh4[Xl? MlLPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OEK2O|EoRjJ|NEiyOlcyRC:jPh?=
Glioblastoma initiating cells Mk\USpVv[3Srb36gZZN{[Xl? NVywfVl6hjFyIN88US=> NUTa[plOUW6qaXLpeJMhfGinIFX4dJJme3Orb36gc4YhT2WwZYOgTY53d2y4ZXSgbY4hVWGrboThbY5qdmdiUHz1dolxd3SnbnP5 M4n3[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEiyOlcyLz5{M{S4NlY4OTxxYU6=
Glioblastoma initiating cells NUTlWnh[TnWwY4Tpc44h[XO|YYm= NVjxSHFWhjFyIN88US=> NGTmXVVKdmirYnn0d{BOd3SrbHn0fUwhUW64YYPpc44tKGGwZDDNbYdz[XSrb36= MkHtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OEK2O|EoRjJ|NEiyOlcyRC:jPh?=
LOX IMVI MofqSpVv[3Srb36gZZN{[Xl? NUP4eIE1OTBizszN NELaTJdFVVOR NYj3XpB7cW6qaXLpeJMhUGWmZ3Xoc4cuT0yLIIDheIh4[Xl? MnnVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ|OUO1PVI2RC:jPh?=
UACC 257 M2LtcmZ2dmO2aX;uJIF{e2G7 MlrpNVAh|ryP MkDLSG1UVw>? NHfkRXJqdmirYnn0d{BJ\WSpZXjv[{1IVElicHH0bJdigQ>? Ml;DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ|OUO1PVI2RC:jPh?=
LOX IMVI MkDsSpVv[3Srb36gZZN{[Xl? NGTIT24yOCEQvF2= NEPEZ2tFVVOR NVXlc2FmcW6mdXPld{BIOSClZXzsJIN6[2ynIHHydoV{fA>? NYjPbVlKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|U6OjVpPkKzPVM2QTJ3PD;hQi=>
UACC 257 M{fEPWZ2dmO2aX;uJIF{e2G7 NXXoeVBOOTBizszN MV3EUXNQ M3rBN4lv\HWlZYOgS|Eh[2WubDDjfYNt\SCjcoLld5Q> MoLxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ|OUO1PVI2RC:jPh?=
LOX IMVI MUfDfZRwgGmlaYT5JIF{e2G7 MX2xNEDPxE1? NUG3WHZXTE2VTx?= NF;R[5hl\WO{ZXHz[ZMhfHWvb4KgZ4VtdCC4aXHibYxqfHl? MmnWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ|OUO1PVI2RC:jPh?=
UACC 257 MX\DfZRwgGmlaYT5JIF{e2G7 NVi3UmV[OTBizszN Mk[4SG1UVw>? MX3k[YNz\WG|ZYOgeJVud3JiY3XscEB3cWGkaXzpeJk> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl|NUmyOUc,OjN7M{W5NlU9N2F-
LOX IMVI NYO2TpZTSXCxcITvd4l{KGG|c3H5 M13MeFExKM7:TR?= M3u1T2ROW09? Mk\5bY5lfWOnczDhdI9xfG:|aYO= M4rye|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUO1PVI2Lz5{M{mzOVkzPTxxYU6=
UACC 257 NWT1U4lNSXCxcITvd4l{KGG|c3H5 NFWyTnIyOCEQvF2= MlTFSG1UVw>? MX3pcoR2[2W|IHHwc5B1d3Orcx?= M{nUfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUO1PVI2Lz5{M{mzOVkzPTxxYU6=
ACHN NHzLe4pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVv4[Y5ohjVizszN M3TMcWROW09? MlvPTWM2OD1{LURihKnPxE1? MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB7M{S5NUc,OjVyOUO0PVE9N2F-
769-P MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnLaglUh|ryP M{jy[GROW09? MV7JR|UxRTJvM,MAje69VQ>? NVrUVoJ2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPVM1QTFpPkK1NFk{PDlzPD;hQi=>
786-O MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{fUfp42KM7:TR?= M1nmPGROW09? MljMTWM2OD1{LURihKnPxE1? M{e4RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEmzOFkyLz5{NUC5N|Q6OTxxYU6=
786-O SuR M2HKXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV[1[I5xhjVizszN MnSxSG1UVw>? NWrES5ZHUUN3ME2yMVPjiIoQvF2= NGq0UpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC5N|Q6OSd-MkWwPVM1QTF:L3G+
SP53 MULGeY5kfGmxbjDhd5NigQ>? Mnn6N|Ah|ryP NETBVYNFVVOR MYXpcohq[mm2czDj[YxtKGGmaHXzbY9vKGGwZDDtbYdz[XSrb36= NGnDWY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki4OVYxQCd-Mk[4PFU3ODh:L3G+
SP53 M4K0OGZ2dmO2aX;uJIF{e2G7 Mk\iN|Ah|ryP NEfLXGpFVVOR NYrJdnp5cW6qaXLpeJMhfGinIG\MRVQudWWmaXH0[YQhTkGNIIPp[45idGmwZzDwZZRpf2G7 M4iy[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OEi1OlA5Lz5{Nki4OVYxQDxxYU6=
HS5 NHrEenJHfW6ldHnvckBie3OjeR?= M{W2RlMxKM7:TR?= NHrCbJVFVVOR M13WTolvcGmkaYTzJINmdGxiYXTo[ZNqd25iYX7kJI1q\3KjdHnvci=> NYm5XGRHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4PFU3ODhpPkK2PFg2PjB6PD;hQi=>
HS27a M1e2SGZ2dmO2aX;uJIF{e2G7 M{S2XlMxKM7:TR?= NV\RWld[TE2VTx?= M{H6UIlvcGmkaYTzJINmdGxiYXTo[ZNqd25iYX7kJI1q\3KjdHnvci=> MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh6NU[wPEc,OjZ6OEW2NFg9N2F-
SP53 NXjRTW1oS3m2b4jpZ4l1gSCjc4PhfS=> NWHFcZFWOzBizszN Mn3aSG1UVw>? MXLpcoR2[2W|IHH1eI9xcGGpeR?= M2rsRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OEi1OlA5Lz5{Nki4OVYxQDxxYU6=
Jeko NFjqbplEgXSxeHnjbZR6KGG|c3H5 M{TIV|MxKM7:TR?= M{HZUmROW09? MmnJbY5lfWOnczDheZRweGijZ4m= MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh6NU[wPEc,OjZ6OEW2NFg9N2F-
U2OS Mly0SpVv[3Srb36gZZN{[Xl? MX[yJIhzew>? MUfEbZNxdGGlZX3lcpQhd2ZiW{PIYYN6[2yxcHHtbY5mKG[{b32ge4lt\CC2eYDlJHNudyCneIDy[ZN{\WRiaX6gWVJQWyClZXzsd{Bi\nSncjCyJIhzeyCkeTDzZ4lvfGmubHH0bY9vKGOxdX70bY5oNCCNaTC9JFAvODB4IN88UU4> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB4M{WyNkc,OjNyNkO1NlI9N2F-
NIH/3T3 NWDzOHBGTnWwY4Tpc44h[XO|YYm= NV\tOJNqUW6qaXLpeIlwdiCxZjDo[YRo\WixZzDzbYdv[WyrbnegdIF1cHejeTDpckBud3W|ZTDOTWgwO1R|IHPlcIx{KGW6cILld5Nqdmdid3ns[EB1gXCnIGPtc{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gS4xqKG2UTlGg[ZhxemW|c3nvckBjgSCUVD3QR3IhdWW2aH;kMEBKSzVyIE2gNE4xODR2IN88UU4> MlXLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd6MUC1PVEoRjJ5OEGwOVkyRC:jPh?=
NIH/3T3 MkDYSpVv[3Srb36gZZN{[Xl? NX7acGxGUW6qaXLpeIlwdiCxZjDo[YRo\WixZzDzbYdv[WyrbnegdIF1cHejeTDpckBud3W|ZTDOTWgwO1R|IHPlcIx{KGijcnLvdolv\yCVbX:gSFQ4P0hibYX0ZY51KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBIdGlibWLORUBmgHC{ZYPzbY9vKGK7IGLUMXBEWiCvZYToc4QtKEmFNUCgQUAxNjB{Mkeg{txONg>? NIXjOZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{ixNFU6OSd-Mke4NVA2QTF:L3G+
NIH/3T3 M3nONWZ2dmO2aX;uJIF{e2G7 NYfEPYp5OjRiaILz Ml;2TY5pcWKrdHnvckBw\iCqZXTn[Yhw\yC|aXfuZYxqdmdicHH0bJdigSCrbjDtc5V{\SCQSVivN3Q{KGOnbHzzJI1m[XO3cnXkJIFnfGW{IEK0JIhzeyCkeTDHcIku\HWjbDDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUCgQUAxNjByNjFOwG0v NIHLW3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{ixNFU6OSd-Mke4NVA2QTF:L3G+
TM3 MYnGeY5kfGmxbjDhd5NigQ>? NEHRS4s1QCCqcoO= MVzJcohq[mm2aX;uJI9nKEiqIIPp[45idGmwZzDwZZRpf2G7IHnuJI1wfXOnIGTNN{Bk\WyuczDhd5Nme3OnZDDhd{Bld3ewcnXneYxifGmxbjDv[kBIdGlzIHflcoUh\XiycnXzd4lwdiCjZoTldkA1QCCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxKD1iMD6wNFEzKM7:TT6= M1XBPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUe2NlE2Lz5{Nkm3OlIyPTxxYU6=
NIH3T3 M1;DW2Z2dmO2aX;uJIF{e2G7 NEfSUFM1QCCqcoO= NEH5R4tKdmirYnn0bY9vKG:oIGPITEB{cWewYXzpcocheGG2aIfhfUBqdiCvb4Xz[UBPUUh|VEOgZ4VtdHNibXXhd5Vz\WRiYX\0[ZIhPDhiaILzJIJ6KEeuaT3seYNq\mW{YYPlJJJmeG:{dHXyJIF{e2G7LDDJR|UxKD1iMD6wNFU2KM7:TT6= MlvOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzN{[zPVYoRjJ2MUe2N|k3RC:jPh?=
NIH3T3 NYr6ZYx7TnWwY4Tpc44h[XO|YYm= NEDPdZM1QCCqcoO= MUXJcohq[mm2aX;uJI9nKFOxbnnjMYlv\HWlZXSgbIVl\2Wqb3egd4lodmGubHnu[{BqdiCvb4Xz[UBPUUh|VEOgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEeuaT3seYNq\mW{YYPlJJJmeG:{dHXyJIF{e2G7LDDJR|UxKD1iMD6wNFU2KM7:TT6= MojIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6MkC1OVQoRjJ4OEKwOVU1RC:jPh?=
NIH/3T3 M4rmTmZ2dmO2aX;uJIF{e2G7 NW\LTGVOUW6qaXLpeIlwdiCxZjDo[YRo\WixZzDzbYdv[WyrbnegdIF1cHejeTDlfJBz\XO|ZXSgbY4hdW:3c3WgUmlJNzOWMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGinZHflbI9oNWmwZIXj[YQhT2yrLUKgZYNkfW23bHH0bY9vKGG2IITpdEBw\iCycnntZZJ6KGOrbHnhJIJ6KESDUFmgd5RicW6rbnegZoF{\WRiY3;u[o9k[WxibXnjdo9{[2:yaXOgZY5idHm|aYO= MoHkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd6MUC1PVEoRjJ5OEGwOVkyRC:jPh?=
NIH/3T3 NGXwdWpHfW6ldHnvckBie3OjeR?= NIjueXpKdmirYnn0bY9vKG:oIHjl[IdmcG:pIIPp[45idGmwZzDwZZRpf2G7IHnuJI1wfXOnIF7JTE8{XDNiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBp\WSpZXjv[{1qdmS3Y3XkJHNudy2HR1\QJINqdGmjcomgeJJidnOub3PheIlwdiCkeTDERXBKKHO2YXnubY5oKGKjc3XkJINwdm[xY3HsJI1q[3Kxc3PvdIlkKGGwYXz5d4l{ NWfJN4xNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke4NVA2QTFpPkK3PFExPTlzPD;hQi=>
MG 63 (6-TG R) MmjTdWhVWyCjc4PhfS=> NFfTUnZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBOTyB4MzCoOk1VTyCUKTDj[Yxtew>? M4rhVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41 MUHxTHRUKGG|c3H5 MWHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSbFQyKGOnbHzz NUOzdI5PRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
U-2 OS MX;xTHRUKGG|c3H5 M2W2[pFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHUuOiCRUzDj[Yxtew>? NF;IemM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
A673 MYLxTHRUKGG|c3H5 NGPGWGxyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= M3;3XFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-12 NVToS5pYeUiWUzDhd5NigQ>? NGDqUY5yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStNVIh[2WubIO= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) M3\hW5FJXFNiYYPzZZk> NW[3[|J1eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz NWTIOWNJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB-EBc1 NWTke4x3eUiWUzDhd5NigQ>? NWTlfI02eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 NGfIeJpyUFSVIHHzd4F6 NFO3OY9yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz NVjFbGVZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 NH;PbXNyUFSVIHHzd4F6 NVzoN|FseUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPhc5MuOiClZXzsdy=> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SJ-GBM2 MknSdWhVWyCjc4PhfS=> Mkf0dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= NFv0VoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC NUTZfYxveUiWUzDhd5NigQ>? MoHQdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= NGXqTIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-SH MWLxTHRUKGG|c3H5 NUP6NYNueUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM> M{G2OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Assay
Methods Test Index PMID
Western blot Bcl2 / c-myc / Cyclin D1 / pERK / ERK / pJNK / JNK / Caspase 3 / Cleaved caspase 3 Gli-1 / Gli-2 / p-Akt / Akt pp70S6K / P70s6k p-p130CAS / p130CAS / p-FAK / FAK / p-Paxillin / Paxillin 22821765 25093491
Immunofluorescence GLI1 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]

  • 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。

动物实验:

[1]

  • 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

溶解度(25°C)

体外

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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

* 必填项

请输入您的姓名
请输入您的邮箱地址 请输入一个有效的邮箱地址
请写点东西给我们