Sonidegib (NVP-LDE225)

Catalog No.S2151 Synonyms: Erismodegib

For research use only.

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.

Sonidegib (NVP-LDE225) Chemical Structure

CAS No. 956697-53-3

Selleck's Sonidegib (NVP-LDE225) has been cited by 49 publications

Purity & Quality Control

Choose Selective Hedgehog/Smoothened Inhibitors

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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 M{DXU2N6fG:6aXPpeJkh[XO|YYm= NGniUm1,OTBizszN NETUV5dKSzVyPUGyJO69VQ>? NGfKZ5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW1N|M2PSd-MkK1OVM{PTV:L3G+
A2780cp20 MoLLR5l1d3irY3n0fUBie3OjeR?= NFr5fJV,OTBizszN MX7JR|UxRTdwNTFOwG0> MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV3M{O1OUc,OjJ3NUOzOVU9N2F-
SKOV3ip1 NUH3O|dmS3m2b4jpZ4l1gSCjc4PhfS=> NXixWm05hjFyIN88US=> MlLITWM2OD1{NDFOwG0> NHuzXZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW1N|M2PSd-MkK1OVM{PTV:L3G+
SKOV3TRip2 MXjDfZRwgGmlaYT5JIF{e2G7 NH\IU4V,OTBizszN M2jObmlEPTB;MUKg{txO MlHPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3NUOzOVUoRjJ{NUWzN|U2RC:jPh?=
HeyA8 NHzXSmdEgXSxeHnjbZR6KGG|c3H5 M4S5bJ4yOCEQvF2= NVnBZZRiUUN3ME2xPEDPxE1? NHzqUGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW1N|M2PSd-MkK1OVM{PTV:L3G+
HeyA8MDR M2G2TGN6fG:6aXPpeJkh[XO|YYm= NUHle5pNhjFyIN88US=> NWLkUVJwUUN3ME24JO69VQ>? MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV3M{O1OUc,OjJ3NUOzOVU9N2F-
OS5 M4q5Umdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MljHglUh|ryP NGPleWxz\WS3Y3XzJJRp\SCycn;sbYZmemG2aX;u M17zS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkSzOVk2Lz5{M{K0N|U6PTxxYU6=
OS18 MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVLwdFBbhjVizszN MW\y[YR2[2W|IITo[UBxem:uaX\ldoF1cW:w NEC0SpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K0N|U6PSd-MkOyOFM2QTV:L3G+
Glioblastoma initiating cells MlfWR5l1d3irY3n0fUBie3OjeR?= NITlUFV,OTBizszN MUfJcohq[mm2czDD[YxtKF[rYXLpcIl1gQ>? NX\IXHVtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0PFI3PzFpPkKzOFgzPjdzPD;hQi=>
Glioblastoma initiating cells NXzyNGYyTnWwY4Tpc44h[XO|YYm= MXX+NVAh|ryP MXLpcohq[mm2czDu[ZVzd3OyaHXy[UBnd3KvYYTpc44> NF63NI09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S4NlY4OSd-MkO0PFI3PzF:L3G+
Glioblastoma initiating cells MojuR5l1d3irY3n0fUBie3OjeR?= NHS4bVh,OTBizszN NH3FSWRqdmS3Y3XzJIFxd3C2b4Ppdy=> MkXTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OEK2O|EoRjJ|NEiyOlcyRC:jPh?=
Glioblastoma initiating cells M3L1V2Z2dmO2aX;uJIF{e2G7 MmnqglExKM7:TR?= NGXBU5Bld3ewcnXneYxifGW|IITo[UBUUEhic3nncoFtcW6pIIDheIh4[Xl? NEj5ZlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S4NlY4OSd-MkO0PFI3PzF:L3G+
Glioblastoma initiating cells MmnGSpVv[3Srb36gZZN{[Xl? MUH+NVAh|ryP NV;tUHNGUW6qaXLpeJMhfGinIFX4dJJme3Orb36gc4YhT2WwZYOgTY53d2y4ZXSgbY4hVWGrboThbY5qdmdiUHz1dolxd3SnbnP5 NF\1fY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S4NlY4OSd-MkO0PFI3PzF:L3G+
Glioblastoma initiating cells M3\ifGZ2dmO2aX;uJIF{e2G7 M1vKN54yOCEQvF2= NF3vNnNKdmirYnn0d{BOd3SrbHn0fUwhUW64YYPpc44tKGGwZDDNbYdz[XSrb36= M33mblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEiyOlcyLz5{M{S4NlY4OTxxYU6=
LOX IMVI NGDmS5RHfW6ldHnvckBie3OjeR?= MnjtNVAh|ryP M1;BdGROW09? NGL3ZYZqdmirYnn0d{BJ\WSpZXjv[{1IVElicHH0bJdigQ>? NEPTS2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{mzOVkzPSd-MkO5N|U6OjV:L3G+
UACC 257 NVT0SmxOTnWwY4Tpc44h[XO|YYm= NEXhT5oyOCEQvF2= MmLVSG1UVw>? M3fxR4lvcGmkaYTzJGhm\GenaH;nMWdNUSCyYYToe4F6 MkX0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ|OUO1PVI2RC:jPh?=
LOX IMVI NX\lXoNmTnWwY4Tpc44h[XO|YYm= Ml21NVAh|ryP MkWzSG1UVw>? M1;1ZYlv\HWlZYOgS|Eh[2WubDDjfYNt\SCjcoLld5Q> M{DUWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUO1PVI2Lz5{M{mzOVkzPTxxYU6=
UACC 257 NHrSSI5HfW6ldHnvckBie3OjeR?= NVzEUJQ1OTBizszN NVfoWpZqTE2VTx?= MkjqbY5lfWOnczDHNUBk\WyuIHP5Z4xmKGG{cnXzeC=> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl|NUmyOUc,OjN7M{W5NlU9N2F-
LOX IMVI MnvFR5l1d3irY3n0fUBie3OjeR?= NXToO3V2OTBizszN NVnScoVYTE2VTx?= NHvYVZNl\WO{ZXHz[ZMhfHWvb4KgZ4VtdCC4aXHibYxqfHl? MmP0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ|OUO1PVI2RC:jPh?=
UACC 257 MYrDfZRwgGmlaYT5JIF{e2G7 MVKxNEDPxE1? M1K2eGROW09? MVfk[YNz\WG|ZYOgeJVud3JiY3XscEB3cWGkaXzpeJk> NGrsXGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{mzOVkzPSd-MkO5N|U6OjV:L3G+
LOX IMVI MnzoRZBweHSxc3nzJIF{e2G7 MnPWNVAh|ryP M1r5TmROW09? MYjpcoR2[2W|IHHwc5B1d3Orcx?= NEK0[IM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{mzOVkzPSd-MkO5N|U6OjV:L3G+
UACC 257 MWDBdI9xfG:|aYOgZZN{[Xl? MlLiNVAh|ryP M3rMVmROW09? NHrCeGRqdmS3Y3XzJIFxd3C2b4Ppdy=> MmfXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ|OUO1PVI2RC:jPh?=
ACHN NFiycpZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXv3NVRVhjVizszN MonDSG1UVw>? M1j3WGlEPTB;Mj2z5qCK|ryP MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB7M{S5NUc,OjVyOUO0PVE9N2F-
769-P MkT6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkPiglUh|ryP MoT1SG1UVw>? M4DhW2lEPTB;Mj2z5qCK|ryP NWLBV5l{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPVM1QTFpPkK1NFk{PDlzPD;hQi=>
786-O NEnKNXZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MX\+OUDPxE1? M4niVmROW09? M3PidWlEPTB;Mj2z5qCK|ryP M2LDdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEmzOFkyLz5{NUC5N|Q6OTxxYU6=
786-O SuR M3LCcGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkS2glUh|ryP MVLEUXNQ NHfHO|JKSzVyPUKtN-KBkc7:TR?= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB7M{S5NUc,OjVyOUO0PVE9N2F-
SP53 M4LaPGZ2dmO2aX;uJIF{e2G7 MV2zNEDPxE1? NUSy[oo{TE2VTx?= NFq2bm9qdmirYnn0d{Bk\WyuIHHkbIV{cW:wIHHu[EBucWe{YYTpc44> MoDkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6OEW2NFgoRjJ4OEi1OlA5RC:jPh?=
SP53 NUn6[IJpTnWwY4Tpc44h[XO|YYm= NGK4bVc{OCEQvF2= MYHEUXNQ MUDpcohq[mm2czD0bIUhXkyDND3t[YRq[XSnZDDGRWshe2mpbnHsbY5oKHCjdHj3ZZk> NFzqSWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki4OVYxQCd-Mk[4PFU3ODh:L3G+
HS5 Mmn4SpVv[3Srb36gZZN{[Xl? NGXMOpI{OCEQvF2= NXX5TXFoTE2VTx?= NV\LR3RCcW6qaXLpeJMh[2WubDDh[Ihme2mxbjDhcoQhdWmpcnH0bY9v Mnz0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6OEW2NFgoRjJ4OEi1OlA5RC:jPh?=
HS27a M3LnfmZ2dmO2aX;uJIF{e2G7 MkPKN|Ah|ryP MmPISG1UVw>? MoPYbY5pcWKrdIOgZ4VtdCCjZHjld4lwdiCjbnSgcYloemG2aX;u MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh6NU[wPEc,OjZ6OEW2NFg9N2F-
SP53 MnzPR5l1d3irY3n0fUBie3OjeR?= NGDLTo0{OCEQvF2= NVX4cnBbTE2VTx?= M2TtfYlv\HWlZYOgZZV1d3CqYXf5 NV;hTYZqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4PFU3ODhpPkK2PFg2PjB6PD;hQi=>
Jeko NYLoW3ZXS3m2b4jpZ4l1gSCjc4PhfS=> MlfBN|Ah|ryP NGjUOmRFVVOR Ml;LbY5lfWOnczDheZRweGijZ4m= M1v5VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OEi1OlA5Lz5{Nki4OVYxQDxxYU6=
U2OS M1vhUGZ2dmO2aX;uJIF{e2G7 M3vSPVIhcHK| MoroSIl{eGyjY3Xt[Y51KG:oIGuzTH1kgWOub4DhcYlv\SCocn;tJJdqdGRidInw[UBUdW9iZYjwdoV{e2WmIHnuJHUzV1NiY3XscJMh[W[2ZYKgNkBpenNiYomgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiS3mgQUAxNjByNjFOwG0v MmG4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyNkO1NlIoRjJ|ME[zOVIzRC:jPh?=
NIH/3T3 MXXGeY5kfGmxbjDhd5NigQ>? M4L1dGlvcGmkaYTpc44hd2ZiaHXk[4Vpd2dic3nncoFtcW6pIIDheIh4[XliaX6gcY92e2ViTlnIM|NVOyClZXzsd{BmgHC{ZYPzbY5oKHerbHSgeJlx\SCVbX:gZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIFfsbUBuWk6DIHX4dJJme3Orb36gZpkhWlRvUFPSJI1mfGixZDygTWM2OCB;IECuNFA1PCEQvF2u NWHsSo11RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke4NVA2QTFpPkK3PFExPTlzPD;hQi=>
NIH/3T3 NH64VFhHfW6ldHnvckBie3OjeR?= NH7VZWZKdmirYnn0bY9vKG:oIHjl[IdmcG:pIIPp[45idGmwZzDwZZRpf2G7IHnuJI1wfXOnIF7JTE8{XDNiY3XscJMhcGG{Yn;ybY5oKFOvbzDEOFc4UCCvdYThcpQh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJGdtcSCvUl7BJIV5eHKnc4Ppc44h[nliUmStVGNTKG2ndHjv[EwhUUN3MDC9JFAvODJ{NzFOwG0v NWXQW2ZsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke4NVA2QTFpPkK3PFExPTlzPD;hQi=>
NIH/3T3 NF;ofpNHfW6ldHnvckBie3OjeR?= MV:yOEBpenN? NGLzXpJKdmirYnn0bY9vKG:oIHjl[IdmcG:pIIPp[45idGmwZzDwZZRpf2G7IHnuJI1wfXOnIF7JTE8{XDNiY3XscJMhdWWjc4Xy[YQh[W[2ZYKgNlQhcHK|IHL5JGdtcS2mdXHsJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiSVO1NEA:KDBwMEC2JO69VS5? M1LpZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OEGwOVkyLz5{N{ixNFU6OTxxYU6=
TM3 M3P0UmZ2dmO2aX;uJIF{e2G7 MX20PEBpenN? MVzJcohq[mm2aX;uJI9nKEiqIIPp[45idGmwZzDwZZRpf2G7IHnuJI1wfXOnIGTNN{Bk\WyuczDhd5Nme3OnZDDhd{Bld3ewcnXneYxifGmxbjDv[kBIdGlzIHflcoUh\XiycnXzd4lwdiCjZoTldkA1QCCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxKD1iMD6wNFEzKM7:TT6= NYLzWItoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5O|YzOTVpPkK2PVc3OjF3PD;hQi=>
NIH3T3 M3rBXGZ2dmO2aX;uJIF{e2G7 MXq0PEBpenN? MVjJcohq[mm2aX;uJI9nKFOKSDDzbYdv[WyrbnegdIF1cHejeTDpckBud3W|ZTDOTWg{XDNiY3XscJMhdWWjc4Xy[YQh[W[2ZYKgOFghcHK|IHL5JGdtcS2udXPp[oVz[XOnIILldI9zfGW{IHHzd4F6NCCLQ{WwJF0hOC5yMEW1JO69VS5? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF5NkO5Okc,OjRzN{[zPVY9N2F-
NIH3T3 NYn5S|FkTnWwY4Tpc44h[XO|YYm= M4HjclQ5KGi{cx?= MofCTY5pcWKrdHnvckBw\iCVb37pZ{1qdmS3Y3XkJIhm\GenaH;nJJNq\26jbHzpcochcW5ibX;1d4UhVkmKM2SzJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCJbHmtcJVkcW[ncnHz[UBz\XCxcoTldkBie3OjeTygTWM2OCB;IECuNFA2PSEQvF2u MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh{MEW1OEc,OjZ6MkC1OVQ9N2F-
NIH/3T3 M3f2N2Z2dmO2aX;uJIF{e2G7 MoDvTY5pcWKrdHnvckBw\iCqZXTn[Yhw\yC|aXfuZYxqdmdicHH0bJdigSCneIDy[ZN{\WRiaX6gcY92e2ViTlnIM|NVOyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJIhm\GenaH;nMYlv\HWlZXSgS4xqNTJiYXPjeY12dGG2aX;uJIF1KHSrcDDv[kBxemmvYYL5JINqdGmjIHL5JGRCWElic4ThbY5qdmdiYnHz[YQh[2:wZn;jZYwhdWmlcn;zZ49xcWNiYX7hcJl{cXN? NVvBZ4sxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke4NVA2QTFpPkK3PFExPTlzPD;hQi=>
NIH/3T3 M3\PRWZ2dmO2aX;uJIF{e2G7 NYXsb3lJUW6qaXLpeIlwdiCxZjDo[YRo\WixZzDzbYdv[WyrbnegdIF1cHejeTDpckBud3W|ZTDOTWgwO1R|IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhcGWmZ3Xoc4cucW6mdXPl[EBUdW9vRVfGVEBkcWyrYYL5JJRz[W6|bH;jZZRqd25iYomgSGFRUSC|dHHpcolv\yCkYYPl[EBkd26ob3PhcEBucWO{b4Pjc5Bq[yCjbnHsfZNqew>? NFHCUGE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{ixNFU6OSd-Mke4NVA2QTF:L3G+
MG 63 (6-TG R) MVzxTHRUKGG|c3H5 MWPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDNS{A3OyBqNj3US{BTMSClZXzsdy=> NVuzfWw2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh41 NEDNWodyUFSVIHHzd4F6 MkHQdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVog1OSClZXzsdy=> MnK5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
U-2 OS MV\xTHRUKGG|c3H5 MXHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDVMVIhV1NiY3XscJM> MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
A673 NX3JNYpOeUiWUzDhd5NigQ>? NEDUNYlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= NF72TJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-12 MX;xTHRUKGG|c3H5 M3TqepFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?= M3TEOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R) M131[ZFJXFNiYYPzZZk> MYPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? NW\GWFNsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB-EBc1 M{nXPZFJXFNiYYPzZZk> MkDTdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6ELVXCZ|Eh[2WubIO= M2G3d|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50 MUDxTHRUKGG|c3H5 MmC5dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= MkLxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 MmDldWhVWyCjc4PhfS=> NV:5b4h{eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPhc5MuOiClZXzsdy=> NFPGfGg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 NVfkS3dEeUiWUzDhd5NigQ>? MXnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= MkPGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC M3;PU5FJXFNiYYPzZZk> NUjpSZJreUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> NYfScFFXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH NGL5Z3ZyUFSVIHHzd4F6 MnLrdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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
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 (from reference)

Cell Research:

[1]

  • 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]

  • 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 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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
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)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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