Sonidegib (NVP-LDE225)

For research use only.

Catalog No.S2151 Synonyms: Erismodegib

44 publications

Sonidegib (NVP-LDE225) Chemical Structure

CAS No. 956697-53-3

Sonidegib (Erismodegib, NVP-LDE225) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human) in cell-free assays, respectively. Phase 3.

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Selleck's Sonidegib (NVP-LDE225) has been cited by 44 publications

Purity & Quality Control

Choose Selective Hedgehog/Smoothened Inhibitors

Biological Activity

Description Sonidegib (Erismodegib, NVP-LDE225) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human) in cell-free assays, respectively. Phase 3.
Targets
Smo (mouse) [1]
(Cell-free assay)
Smo (human) [1]
(Cell-free assay)
1.3 nM 2.5 nM
In vitro

Sonidegib (Erismodegib, NVP-LDE225) inhibits TM3 luciferized cell line with 0.6 nM and 8 nM, at the presence of 1 nM and 25 nM Hh agonist Ag1.5, respectively. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A2780ip2 MoXsR5l1d3irY3n0fUBie3OjeR?= MWj+NVAh|ryP NHfNbWJKSzVyPUGyJO69VQ>? NWPGSXkzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1OVM{PTVpPkKyOVU{OzV3PD;hQi=>
A2780cp20 M3\CcWN6fG:6aXPpeJkh[XO|YYm= MUj+NVAh|ryP MYjJR|UxRTdwNTFOwG0> M{[5W|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUWzN|U2Lz5{MkW1N|M2PTxxYU6=
SKOV3ip1 MXLDfZRwgGmlaYT5JIF{e2G7 MkmyglExKM7:TR?= Ml\zTWM2OD1{NDFOwG0> M37tRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUWzN|U2Lz5{MkW1N|M2PTxxYU6=
SKOV3TRip2 MWXDfZRwgGmlaYT5JIF{e2G7 NH75dGx,OTBizszN NXHUdYJrUUN3ME2xNkDPxE1? MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV3M{O1OUc,OjJ3NUOzOVU9N2F-
HeyA8 NIniUnlEgXSxeHnjbZR6KGG|c3H5 NXLwe406hjFyIN88US=> MkG0TWM2OD1zODFOwG0> MnS3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3NUOzOVUoRjJ{NUWzN|U2RC:jPh?=
HeyA8MDR NULVUYE3S3m2b4jpZ4l1gSCjc4PhfS=> M4THVJ4yOCEQvF2= NHHPbnpKSzVyPUig{txO MlfKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3NUOzOVUoRjJ{NUWzN|U2RC:jPh?=
OS5 Mn\ZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHPPN2F,PSEQvF2= NHHWdZBz\WS3Y3XzJJRp\SCycn;sbYZmemG2aX;u NELLepI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K0N|U6PSd-MkOyOFM2QTV:L3G+
OS18 Mn;JS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NELESZR,PSEQvF2= MWHy[YR2[2W|IITo[UBxem:uaX\ldoF1cW:w MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ2M{W5OUc,OjN{NEO1PVU9N2F-
Glioblastoma initiating cells MYDDfZRwgGmlaYT5JIF{e2G7 MUL+NVAh|ryP Ml7xTY5pcWKrdIOgR4VtdCCYaXHibYxqfHl? MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR6Mk[3NUc,OjN2OEK2O|E9N2F-
Glioblastoma initiating cells M3:2emZ2dmO2aX;uJIF{e2G7 MnPHglExKM7:TR?= Mny4bY5pcWKrdIOgcoV2em:|cHjldoUh\m:{bXH0bY9v NV\kdGV[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0PFI3PzFpPkKzOFgzPjdzPD;hQi=>
Glioblastoma initiating cells NX\kcXpzS3m2b4jpZ4l1gSCjc4PhfS=> MVn+NVAh|ryP NFToN2pqdmS3Y3XzJIFxd3C2b4Ppdy=> NU\wXGU2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0PFI3PzFpPkKzOFgzPjdzPD;hQi=>
Glioblastoma initiating cells MniwSpVv[3Srb36gZZN{[Xl? NFPKbYF,OTBizszN NY\seJdH\G:5boLl[5Vt[XSnczD0bIUhW0iKIIPp[45idGmwZzDwZZRpf2G7 MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR6Mk[3NUc,OjN2OEK2O|E9N2F-
Glioblastoma initiating cells MlrTSpVv[3Srb36gZZN{[Xl? M{HYXJ4yOCEQvF2= MXfJcohq[mm2czD0bIUhTXiycnXzd4lwdiCxZjDH[Y5meyCLbo\vcJZm\CCrbjDNZYlvfGGrbnnu[{BRdHW{aYDveIVv[3l? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR6Mk[3NUc,OjN2OEK2O|E9N2F-
Glioblastoma initiating cells MVHGeY5kfGmxbjDhd5NigQ>? NH\uUXh,OTBizszN NUi4O3hbUW6qaXLpeJMhVW:2aXzpeJktKEmwdnHzbY9vNCCjbnSgUYloemG2aX;u NGPC[Wc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S4NlY4OSd-MkO0PFI3PzF:L3G+
LOX IMVI NHnBNIlHfW6ldHnvckBie3OjeR?= NGXxNWoyOCEQvF2= NX[yS5N3TE2VTx?= M{S2folvcGmkaYTzJGhm\GenaH;nMWdNUSCyYYToe4F6 MkG2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ|OUO1PVI2RC:jPh?=
UACC 257 MnPpSpVv[3Srb36gZZN{[Xl? M3nzU|ExKM7:TR?= NUPCU2tVTE2VTx?= NHG3blFqdmirYnn0d{BJ\WSpZXjv[{1IVElicHH0bJdigQ>? Ml\JQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ|OUO1PVI2RC:jPh?=
LOX IMVI Mk\LSpVv[3Srb36gZZN{[Xl? MYSxNEDPxE1? M{fzcWROW09? NFvIdFRqdmS3Y3XzJGcyKGOnbHygZ5lkdGViYYLy[ZN1 Mn7xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ|OUO1PVI2RC:jPh?=
UACC 257 MXrGeY5kfGmxbjDhd5NigQ>? MWmxNEDPxE1? NWWy[Yl7TE2VTx?= M3O1UIlv\HWlZYOgS|Eh[2WubDDjfYNt\SCjcoLld5Q> NHP4RXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{mzOVkzPSd-MkO5N|U6OjV:L3G+
LOX IMVI NVK4VG8yS3m2b4jpZ4l1gSCjc4PhfS=> Mmn4NVAh|ryP NI[0ZY5FVVOR NYmz[3Ry\GWlcnXhd4V{KHS3bX;yJINmdGxidnnhZoltcXS7 M1HjXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUO1PVI2Lz5{M{mzOVkzPTxxYU6=
UACC 257 MX3DfZRwgGmlaYT5JIF{e2G7 MXGxNEDPxE1? MmKySG1UVw>? MlPp[IVkemWjc3XzJJR2dW:{IHPlcIwhfmmjYnnsbZR6 MkG2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ|OUO1PVI2RC:jPh?=
LOX IMVI M4[xc2Fxd3C2b4Ppd{Bie3OjeR?= Mn\QNVAh|ryP NVG4VoVwTE2VTx?= NFfhb5lqdmS3Y3XzJIFxd3C2b4Ppdy=> M{niSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUO1PVI2Lz5{M{mzOVkzPTxxYU6=
UACC 257 NWn3TVF6SXCxcITvd4l{KGG|c3H5 MX[xNEDPxE1? Ml\jSG1UVw>? NUjUZlZZcW6mdXPld{BieG:ydH;zbZM> NYfvXHRURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|U6OjVpPkKzPVM2QTJ3PD;hQi=>
ACHN Mn3XS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NETwdnZ,PSEQvF2= NWe3XJJVTE2VTx?= NFvBNXVKSzVyPUKtN-KBkc7:TR?= NXjsTFRiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPVM1QTFpPkK1NFk{PDlzPD;hQi=>
769-P NHGxcJZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXPkeFVphjVizszN NYfW[np1TE2VTx?= NITJeWJKSzVyPUKtN-KBkc7:TR?= M4P6NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEmzOFkyLz5{NUC5N|Q6OTxxYU6=
786-O M1jZNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmHQglUh|ryP MoOzSG1UVw>? MYfJR|UxRTJvM,MAje69VQ>? NF3pOms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC5N|Q6OSd-MkWwPVM1QTF:L3G+
786-O SuR MVHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1:2ZZ42KM7:TR?= NIe5XopFVVOR NH\wT|VKSzVyPUKtN-KBkc7:TR?= M2XjOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEmzOFkyLz5{NUC5N|Q6OTxxYU6=
SP53 NWTnSYJ1TnWwY4Tpc44h[XO|YYm= MUSzNEDPxE1? MmPRSG1UVw>? NHv3OIdqdmirYnn0d{Bk\WyuIHHkbIV{cW:wIHHu[EBucWe{YYTpc44> NVLhfVY4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4PFU3ODhpPkK2PFg2PjB6PD;hQi=>
SP53 MkT5SpVv[3Srb36gZZN{[Xl? Mnn1N|Ah|ryP NGDn[VJFVVOR MkHlbY5pcWKrdIOgeIhmKF[OQUStcYVlcWG2ZXSgSmFMKHOrZ37hcIlv\yCyYYToe4F6 MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh6NU[wPEc,OjZ6OEW2NFg9N2F-
HS5 M{\temZ2dmO2aX;uJIF{e2G7 NGPZUI4{OCEQvF2= M1H6cmROW09? MY\pcohq[mm2czDj[YxtKGGmaHXzbY9vKGGwZDDtbYdz[XSrb36= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh6NU[wPEc,OjZ6OEW2NFg9N2F-
HS27a Mn3mSpVv[3Srb36gZZN{[Xl? NEizemM{OCEQvF2= NWnmb5RoTE2VTx?= NXnpUHZNcW6qaXLpeJMh[2WubDDh[Ihme2mxbjDhcoQhdWmpcnH0bY9v NGfzbIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki4OVYxQCd-Mk[4PFU3ODh:L3G+
SP53 M{D1NWN6fG:6aXPpeJkh[XO|YYm= M{S5[|MxKM7:TR?= NX3YdmdYTE2VTx?= NIDSc3VqdmS3Y3XzJIF2fG:yaHHnfS=> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh6NU[wPEc,OjZ6OEW2NFg9N2F-
Jeko MV\DfZRwgGmlaYT5JIF{e2G7 NUfSbJVtOzBizszN MVzEUXNQ NHLxT|dqdmS3Y3XzJIF2fG:yaHHnfS=> NVfyVos4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4PFU3ODhpPkK2PFg2PjB6PD;hQi=>
U2OS NWTRVHVFTnWwY4Tpc44h[XO|YYm= M4TlcFIhcHK| NGfQS5pFcXOybHHj[Y1mdnRib3[gX|NJZWO7Y3zvdIFucW6nIH\yc40hf2muZDD0fZBmKFOvbzDlfJBz\XO|ZXSgbY4hXTKRUzDj[YxteyCjZoTldkAzKGi{czDifUB{[2mwdHnscIF1cW:wIHPveY51cW6pLDDLbUA:KDBwMEC2JO69VS5? NFjveIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{C2N|UzOid-MkOwOlM2OjJ:L3G+
NIH/3T3 NXfLOoJkTnWwY4Tpc44h[XO|YYm= NIqxWnVKdmirYnn0bY9vKG:oIHjl[IdmcG:pIIPp[45idGmwZzDwZZRpf2G7IHnuJI1wfXOnIF7JTE8{XDNiY3XscJMh\XiycnXzd4lv\yC5aXzkJJR6eGViU33vJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDHcIkhdVKQQTDlfJBz\XO|aX;uJIJ6KFKWLWDDVkBu\XSqb3SsJGlEPTBiPTCwMlAxPDRizszNMi=> NGSzR2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{ixNFU6OSd-Mke4NVA2QTF:L3G+
NIH/3T3 NFrEW|hHfW6ldHnvckBie3OjeR?= MnXrTY5pcWKrdHnvckBw\iCqZXTn[Yhw\yC|aXfuZYxqdmdicHH0bJdigSCrbjDtc5V{\SCQSVivN3Q{KGOnbHzzJIhiemKxcnnu[{BUdW9iRES3O2ghdXW2YX70JIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDHcIkhdVKQQTDlfJBz\XO|aX;uJIJ6KFKWLWDDVkBu\XSqb3SsJGlEPTBiPTCwMlAzOjdizszNMi=> M1y5eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OEGwOVkyLz5{N{ixNFU6OTxxYU6=
NIH/3T3 M1fTc2Z2dmO2aX;uJIF{e2G7 Mof6NlQhcHK| M2PHNmlvcGmkaYTpc44hd2ZiaHXk[4Vpd2dic3nncoFtcW6pIIDheIh4[XliaX6gcY92e2ViTlnIM|NVOyClZXzsd{Bu\WG|dYLl[EBi\nSncjCyOEBpenNiYomgS4xqNWS3YXygcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwJF0hOC5yME[g{txONg>? MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzhzMEW5NUc,Ojd6MUC1PVE9N2F-
TM3 NV\EeWtOTnWwY4Tpc44h[XO|YYm= NX;HRml4PDhiaILz NFXYV2ZKdmirYnn0bY9vKG:oIFjoJJNq\26jbHnu[{Bx[XSqd3H5JIlvKG2xdYPlJHROOyClZXzsd{Bie3Onc4Pl[EBieyCmb4fudoVofWyjdHnvckBw\iCJbHmxJIdmdmViZYjwdoV{e2mxbjDh[pRmeiB2ODDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyIE2gNE4xODF{IN88UU4> MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl5NkKxOUc,OjZ7N{[yNVU9N2F-
NIH3T3 MnzlSpVv[3Srb36gZZN{[Xl? MknEOFghcHK| M3vW[2lvcGmkaYTpc44hd2ZiU1jIJJNq\26jbHnu[{Bx[XSqd3H5JIlvKG2xdYPlJG5KUDOWMzDj[YxteyCvZXHzeZJm\CCjZoTldkA1QCCqcoOgZpkhT2yrLXz1Z4ln\XKjc3WgdoVxd3K2ZYKgZZN{[XluIFnDOVAhRSByLkCwOVUh|ryPLh?= M4i1PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUe2N|k3Lz5{NEG3OlM6PjxxYU6=
NIH3T3 NUHuNm05TnWwY4Tpc44h[XO|YYm= NFf5XHI1QCCqcoO= MVHJcohq[mm2aX;uJI9nKFOxbnnjMYlv\HWlZXSgbIVl\2Wqb3egd4lodmGubHnu[{BqdiCvb4Xz[UBPUUh|VEOgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEeuaT3seYNq\mW{YYPlJJJmeG:{dHXyJIF{e2G7LDDJR|UxKD1iMD6wNFU2KM7:TT6= MnjSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6MkC1OVQoRjJ4OEKwOVU1RC:jPh?=
NIH/3T3 M3faOGZ2dmO2aX;uJIF{e2G7 NV35eok6UW6qaXLpeIlwdiCxZjDo[YRo\WixZzDzbYdv[WyrbnegdIF1cHejeTDlfJBz\XO|ZXSgbY4hdW:3c3WgUmlJNzOWMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGinZHflbI9oNWmwZIXj[YQhT2yrLUKgZYNkfW23bHH0bY9vKGG2IITpdEBw\iCycnntZZJ6KGOrbHnhJIJ6KESDUFmgd5RicW6rbnegZoF{\WRiY3;u[o9k[WxibXnjdo9{[2:yaXOgZY5idHm|aYO= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzhzMEW5NUc,Ojd6MUC1PVE9N2F-
NIH/3T3 M3zsXmZ2dmO2aX;uJIF{e2G7 Ml33TY5pcWKrdHnvckBw\iCqZXTn[Yhw\yC|aXfuZYxqdmdicHH0bJdigSCrbjDtc5V{\SCQSVivN3Q{KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gbIVl\2Wqb3etbY5lfWOnZDDTcY8uTUeIUDDjbYxq[XK7IITyZY5{dG:lYYTpc44h[nliRFHQTUB{fGGrbnnu[{Bj[XOnZDDjc45nd2OjbDDtbYNzd3Olb4DpZ{BidmGueYPpdy=> M123PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OEGwOVkyLz5{N{ixNFU6OTxxYU6=
MG 63 (6-TG R) NF;nN2xyUFSVIHHzd4F6 MofadWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgUWchPjNiKE[tWGchWiliY3XscJM> NVrIWZQxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh41 M4HQN5FJXFNiYYPzZZk> NXewWXdleUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>? MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
U-2 OS NYLvRpBveUiWUzDhd5NigQ>? MlPFdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWU0zKE:VIHPlcIx{ NEDsV4I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
A673 Ml7XdWhVWyCjc4PhfS=> MV3xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? NEfpZYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-12 Mnz1dWhVWyCjc4PhfS=> MnnQdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| NEf3Wpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
MG 63 (6-TG R) NELBTHZyUFSVIHHzd4F6 M120bpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCPRzC2N{ApPi2WRzDSLUBk\Wyucx?= NFHsfGE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 NHq4dYNyUFSVIHHzd4F6 NYnnc2JkeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> Mm\pQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 MkDmdWhVWyCjc4PhfS=> MkHGdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= M{\URlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Saos-2 NUOycmZ[eUiWUzDhd5NigQ>? MX;xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SJ-GBM2 NXnlWFBHeUiWUzDhd5NigQ>? M4W3dpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz NEP5SpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC NY\pW5NEeUiWUzDhd5NigQ>? MXXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= NXjKUFNLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH NEHYVWxyUFSVIHHzd4F6 NXSzcGZOeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM> NUSw[Y5xRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>

... 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
In vivo Sonidegib (Erismodegib, NVP-LDE225) is highly bound to mouse, rat, and human plasma proteins (>99%) and moderately bound to dog and monkey plasma proteins (77 and 85%, respectively). LDE225 has high permeability (90.8% in man) in the PAMPA assay. LDE225 shows good oral bioavailability ranging from 69 to 102% in preclinical species when dosed in solution. LDE225 is a weak base with a measured pKa of 4.20 and exhibits relatively poor aqueous solubility. LDE225 demonstrates dose-related antitumor activity. At a dose of 5 mg/kg/day qd, LDE225 significantly inhibits tumor growth, corresponding to a T/C value of 33%. When dosed at 10 and 20 mg/kg/day qd, LDE225 gives rise to 51 and 83% regression, respectively. Gli1 mRNA inhibition correlates with tumor and plasma exposure of LDE225. LDE225 successfully penetrates the blood−brain barrier in tumor-bearing animals and results in tumor growth inhibition after 4 days of treatment. [1] LDE225 significantly reduces the tumor volume by 95.7% in Rip1-Tag2 mice. LDE225 prolongs survival in Rip1Tag2 mice. LDE225 decreases expression of stromal markers in the LDE225-treated mice. [2]

Protocol

Cell Research:

[1]

- Collapse
  • Cell lines: TM3Hh12 cells
  • Concentrations: ~10 μM
  • Incubation Time: 30 minutes
  • Method:

    LDE225 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 cultured in F12 Ham's/DMEM (1:1) containing 5% horse serum, 2.5% fetal bovine serum (FBS), and 15 mM HEPES, pH 7.3. Cells are harvested by trypsin treatment, resuspended in F12 Ham's/DMEM (1:1) containing 5% horse serum and 15 mM HEPES, pH 7.3, added to assay plates, and incubated with LDE225 for approximately 30 min at 37 °C in 5% CO2. Then 1 nM or 25 nM Ag1.5 is 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 values, defined as the inflection point of the logistic curve, are determined by nonlinear regression of the Gli-driven luciferase luminescence or absorbance signal from MTS assay vs log10 (concentration) of LDE225 using the R statistical software pack


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • Animal Models: Orthotopic Ptch+/-p53-/- medulloblastoma allograft model in athymic nude mice
  • Dosages: 40 mg/kg/day
  • Administration: Administered via p.o. or b.i.d
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 97 mg/mL (199.79 mM)
Ethanol 97 mg/mL warmed (199.79 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+corn oil
For best results, use promptly after mixing.
10mg/mL

* 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.

Chemical Information

Molecular Weight 485.5
Formula

C26H26F3N3O3

CAS No. 956697-53-3
Storage powder
in solvent
Synonyms Erismodegib
Smiles CC1CN(CC(O1)C)C2=NC=C(C=C2)NC(=O)C3=CC=CC(=C3C)C4=CC=C(C=C4)OC(F)(F)F

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Bio Calculators

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Dilution Calculator

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Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Mass Concentration Volume Molecular Weight

Clinical Trial Information

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
NCT02111187 Completed Drug: LDE225 Prostate Cancer Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins April 2014 Phase 1
NCT02086513 Terminated Drug: LDE225 Graft Versus Host Disease Massachusetts General Hospital|Novartis April 2014 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID