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 52 publications

Purity & Quality Control

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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 M1TSOmN6fG:6aXPpeJkh[XO|YYm= MWj+NVAh|ryP M1X0VmlEPTB;MUKg{txO NXm5UG46RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1OVM{PTVpPkKyOVU{OzV3PD;hQi=>
A2780cp20 MVTDfZRwgGmlaYT5JIF{e2G7 NG\JVYx,OTBizszN MYXJR|UxRTdwNTFOwG0> M2nISFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUWzN|U2Lz5{MkW1N|M2PTxxYU6=
SKOV3ip1 NFLaenZEgXSxeHnjbZR6KGG|c3H5 NWLRNpo5hjFyIN88US=> NYLERZdGUUN3ME2yOEDPxE1? NH3TcpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW1N|M2PSd-MkK1OVM{PTV:L3G+
SKOV3TRip2 Mo\jR5l1d3irY3n0fUBie3OjeR?= M4G1eZ4yOCEQvF2= M3\DNmlEPTB;MUKg{txO NGDpflA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW1N|M2PSd-MkK1OVM{PTV:L3G+
HeyA8 MWHDfZRwgGmlaYT5JIF{e2G7 MnfLglExKM7:TR?= NHXrcVBKSzVyPUG4JO69VQ>? MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV3M{O1OUc,OjJ3NUOzOVU9N2F-
HeyA8MDR MlT6R5l1d3irY3n0fUBie3OjeR?= MX3+NVAh|ryP NH3me5FKSzVyPUig{txO M{PibFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUWzN|U2Lz5{MkW1N|M2PTxxYU6=
OS5 MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFrQOox,PSEQvF2= NGLpSGhz\WS3Y3XzJJRp\SCycn;sbYZmemG2aX;u M1HSfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkSzOVk2Lz5{M{K0N|U6PTxxYU6=
OS18 MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M37Fcp42KM7:TR?= NWntPVNZemWmdXPld{B1cGVicILvcIln\XKjdHnvci=> MlT2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{NEO1PVUoRjJ|MkSzOVk2RC:jPh?=
Glioblastoma initiating cells MWrDfZRwgGmlaYT5JIF{e2G7 M4n5Zp4yOCEQvF2= MlzSTY5pcWKrdIOgR4VtdCCYaXHibYxqfHl? Mn7YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OEK2O|EoRjJ|NEiyOlcyRC:jPh?=
Glioblastoma initiating cells NGD1OWRHfW6ldHnvckBie3OjeR?= MUH+NVAh|ryP MYDpcohq[mm2czDu[ZVzd3OyaHXy[UBnd3KvYYTpc44> NUXlUllCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0PFI3PzFpPkKzOFgzPjdzPD;hQi=>
Glioblastoma initiating cells NXT4NXF4S3m2b4jpZ4l1gSCjc4PhfS=> M3nyfp4yOCEQvF2= NFrOWXZqdmS3Y3XzJIFxd3C2b4Ppdy=> MojjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OEK2O|EoRjJ|NEiyOlcyRC:jPh?=
Glioblastoma initiating cells MVzGeY5kfGmxbjDhd5NigQ>? M{jkUZ4yOCEQvF2= Mmjk[I94dnKnZ4XsZZRmeyC2aHWgV2hJKHOrZ37hcIlv\yCyYYToe4F6 NWjsNno6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0PFI3PzFpPkKzOFgzPjdzPD;hQi=>
Glioblastoma initiating cells NWjFNWh1TnWwY4Tpc44h[XO|YYm= MmDoglExKM7:TR?= MnThTY5pcWKrdIOgeIhmKEW6cILld5Nqd25ib3[gS4Vv\XNiSX72c4x3\WRiaX6gUYFqdnSjaX7pcochWGy3cnnwc5RmdmO7 MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR6Mk[3NUc,OjN2OEK2O|E9N2F-
Glioblastoma initiating cells MVLGeY5kfGmxbjDhd5NigQ>? M2H6cp4yOCEQvF2= M1n3SmlvcGmkaYTzJG1wfGmuaYT5MEBKdn[jc3nvckwh[W6mIF3p[5JifGmxbh?= M{f0UFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEiyOlcyLz5{M{S4NlY4OTxxYU6=
LOX IMVI MXrGeY5kfGmxbjDhd5NigQ>? NY\OOI5POTBizszN NYLyTZJKTE2VTx?= M3Pt[4lvcGmkaYTzJGhm\GenaH;nMWdNUSCyYYToe4F6 Mk\rQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ|OUO1PVI2RC:jPh?=
UACC 257 NVfyeWE6TnWwY4Tpc44h[XO|YYm= MW[xNEDPxE1? NEHXRllFVVOR MUTpcohq[mm2czDI[YRo\WixZz3HUGkheGG2aIfhfS=> MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl|NUmyOUc,OjN7M{W5NlU9N2F-
LOX IMVI NVu0NVBoTnWwY4Tpc44h[XO|YYm= NW[2blZXOTBizszN MVnEUXNQ MofBbY5lfWOnczDHNUBk\WyuIHP5Z4xmKGG{cnXzeC=> NXTMNm5KRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|U6OjVpPkKzPVM2QTJ3PD;hQi=>
UACC 257 MlHzSpVv[3Srb36gZZN{[Xl? NFPCZ2oyOCEQvF2= M3vPTmROW09? NUP0[GpPcW6mdXPld{BIOSClZXzsJIN6[2ynIHHydoV{fA>? MkXjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ|OUO1PVI2RC:jPh?=
LOX IMVI M4Xwe2N6fG:6aXPpeJkh[XO|YYm= MUSxNEDPxE1? MV7EUXNQ NHezOYhl\WO{ZXHz[ZMhfHWvb4KgZ4VtdCC4aXHibYxqfHl? MojKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ|OUO1PVI2RC:jPh?=
UACC 257 M4DTRmN6fG:6aXPpeJkh[XO|YYm= NYju[IFXOTBizszN NUfVTIE{TE2VTx?= NEjvWlFl\WO{ZXHz[ZMhfHWvb4KgZ4VtdCC4aXHibYxqfHl? M{frcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUO1PVI2Lz5{M{mzOVkzPTxxYU6=
LOX IMVI MmjTRZBweHSxc3nzJIF{e2G7 NWHnNHVuOTBizszN M{G4UWROW09? NHfHZ3hqdmS3Y3XzJIFxd3C2b4Ppdy=> NFTG[lk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{mzOVkzPSd-MkO5N|U6OjV:L3G+
UACC 257 NHnnbG9CeG:ydH;zbZMh[XO|YYm= NFnqc24yOCEQvF2= NYXONotOTE2VTx?= MVLpcoR2[2W|IHHwc5B1d3Orcx?= NUmxemd{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|U6OjVpPkKzPVM2QTJ3PD;hQi=>
ACHN MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWXsXFdRhjVizszN M2jxSGROW09? MnzPTWM2OD1{LURihKnPxE1? NYnjeI1jRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPVM1QTFpPkK1NFk{PDlzPD;hQi=>
769-P Moj4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVzSWIJnhjVizszN Mm\wSG1UVw>? MkT0TWM2OD1{LURihKnPxE1? M3XFcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEmzOFkyLz5{NUC5N|Q6OTxxYU6=
786-O M3vSO2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3;uPJ42KM7:TR?= M4G5cmROW09? Mmr4TWM2OD1{LURihKnPxE1? NX6xc4VlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPVM1QTFpPkK1NFk{PDlzPD;hQi=>
786-O SuR NGfBXnNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYTCW4xthjVizszN M2nOb2ROW09? NUOzRVNlUUN3ME2yMVPjiIoQvF2= Ml76QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyOUO0PVEoRjJ3MEmzOFkyRC:jPh?=
SP53 NHPqNnRHfW6ldHnvckBie3OjeR?= MYCzNEDPxE1? M2SzTmROW09? MlfCbY5pcWKrdIOgZ4VtdCCjZHjld4lwdiCjbnSgcYloemG2aX;u M{LWVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OEi1OlA5Lz5{Nki4OVYxQDxxYU6=
SP53 MVrGeY5kfGmxbjDhd5NigQ>? M3LZdlMxKM7:TR?= M2LX[2ROW09? M{TOWolvcGmkaYTzJJRp\SCYTFG0MY1m\GmjdHXkJGZCUyC|aXfuZYxqdmdicHH0bJdigQ>? MnjFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6OEW2NFgoRjJ4OEi1OlA5RC:jPh?=
HS5 NUP5SnI4TnWwY4Tpc44h[XO|YYm= M1e5T|MxKM7:TR?= MUXEUXNQ NXTDT4ZxcW6qaXLpeJMh[2WubDDh[Ihme2mxbjDhcoQhdWmpcnH0bY9v NWW4c4VbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4PFU3ODhpPkK2PFg2PjB6PD;hQi=>
HS27a NYXuVlVZTnWwY4Tpc44h[XO|YYm= MljkN|Ah|ryP MX;EUXNQ MmnmbY5pcWKrdIOgZ4VtdCCjZHjld4lwdiCjbnSgcYloemG2aX;u NXz6UVViRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4PFU3ODhpPkK2PFg2PjB6PD;hQi=>
SP53 MkXqR5l1d3irY3n0fUBie3OjeR?= MlfIN|Ah|ryP M3v2e2ROW09? MoXLbY5lfWOnczDheZRweGijZ4m= MmXYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6OEW2NFgoRjJ4OEi1OlA5RC:jPh?=
Jeko MnLrR5l1d3irY3n0fUBie3OjeR?= M3TseFMxKM7:TR?= M4XMVWROW09? NGnNNllqdmS3Y3XzJIF2fG:yaHHnfS=> MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh6NU[wPEc,OjZ6OEW2NFg9N2F-
U2OS M4DlOGZ2dmO2aX;uJIF{e2G7 M{DIRVIhcHK| NUHnfVhFTGm|cHzhZ4Vu\W62IH;mJHs{UF2leXPsc5BidWmwZTDmdo9uKHerbHSgeJlx\SCVbX:g[ZhxemW|c3XkJIlvKFV{T2OgZ4VtdHNiYX\0[ZIhOiCqcoOgZpkhe2OrboTpcIxifGmxbjDjc5VvfGmwZzygT4khRSByLkCwOkDPxE1w M1jocVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|ME[zOVIzLz5{M{C2N|UzOjxxYU6=
NIH/3T3 NH3PV|FHfW6ldHnvckBie3OjeR?= MULJcohq[mm2aX;uJI9nKGinZHflbI9oKHOrZ37hcIlv\yCyYYToe4F6KGmwIH3veZNmKE6LSD:zWFMh[2WubIOg[ZhxemW|c3nu[{B4cWymIIT5dIUhW22xIHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCJbHmgcXJPSSCneIDy[ZN{cW:wIHL5JHJVNVCFUjDt[ZRpd2RuIFnDOVAhRSByLkCwOFQh|ryPLh?= NXHqdIxORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke4NVA2QTFpPkK3PFExPTlzPD;hQi=>
NIH/3T3 NG\LWXZHfW6ldHnvckBie3OjeR?= NHjvcXlKdmirYnn0bY9vKG:oIHjl[IdmcG:pIIPp[45idGmwZzDwZZRpf2G7IHnuJI1wfXOnIF7JTE8{XDNiY3XscJMhcGG{Yn;ybY5oKFOvbzDEOFc4UCCvdYThcpQh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJGdtcSCvUl7BJIV5eHKnc4Ppc44h[nliUmStVGNTKG2ndHjv[EwhUUN3MDC9JFAvODJ{NzFOwG0v NF\CcVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{ixNFU6OSd-Mke4NVA2QTF:L3G+
NIH/3T3 NHHwd5RHfW6ldHnvckBie3OjeR?= NFviOJUzPCCqcoO= NE\Vc|JKdmirYnn0bY9vKG:oIHjl[IdmcG:pIIPp[45idGmwZzDwZZRpf2G7IHnuJI1wfXOnIF7JTE8{XDNiY3XscJMhdWWjc4Xy[YQh[W[2ZYKgNlQhcHK|IHL5JGdtcS2mdXHsJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiSVO1NEA:KDBwMEC2JO69VS5? NXrGb5VKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke4NVA2QTFpPkK3PFExPTlzPD;hQi=>
TM3 MVvGeY5kfGmxbjDhd5NigQ>? MWK0PEBpenN? NVfwPIZ2UW6qaXLpeIlwdiCxZjDIbEB{cWewYXzpcocheGG2aIfhfUBqdiCvb4Xz[UBVVTNiY3XscJMh[XO|ZYPz[YQh[XNiZH;3cpJm\3WuYYTpc44hd2ZiR3zpNUBo\W6nIHX4dJJme3Orb36gZYZ1\XJiNEigbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3MDC9JFAvODBzMjFOwG0v NVm1WmtJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5O|YzOTVpPkK2PVc3OjF3PD;hQi=>
NIH3T3 NFvtXVJHfW6ldHnvckBie3OjeR?= MnjIOFghcHK| MkK0TY5pcWKrdHnvckBw\iCVSFigd4lodmGuaX7nJJBifGi5YYmgbY4hdW:3c3WgUmlJO1R|IHPlcIx{KG2nYYP1doVlKGGodHXyJFQ5KGi{czDifUBIdGlvbIXjbYZmemG|ZTDy[ZBwenSncjDhd5NigSxiSVO1NEA:KDBwMEC1OUDPxE1w NXXLUGVbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxO|Y{QTZpPkK0NVc3Ozl4PD;hQi=>
NIH3T3 MmL4SpVv[3Srb36gZZN{[Xl? MXm0PEBpenN? NF7CSWJKdmirYnn0bY9vKG:oIGPvcolkNWmwZIXj[YQhcGWmZ3Xoc4che2mpbnHscIlv\yCrbjDtc5V{\SCQSVizWFMh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFfsbU1tfWOrZnXyZZNmKHKncH;yeIVzKGG|c3H5MEBKSzVyIE2gNE4xODV3IN88UU4> NETn[Xc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkiyNFU2PCd-Mk[4NlA2PTR:L3G+
NIH/3T3 NHvwcGVHfW6ldHnvckBie3OjeR?= MWHJcohq[mm2aX;uJI9nKGinZHflbI9oKHOrZ37hcIlv\yCyYYToe4F6KGW6cILld5Nm\CCrbjDtc5V{\SCQSVivN3Q{KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gbIVl\2Wqb3etbY5lfWOnZDDHcIkuOiCjY3P1cZVt[XSrb36gZZQhfGmyIH;mJJBzcW2jcomgZ4ltcWFiYomgSGFRUSC|dHHpcolv\yCkYYPl[EBkd26ob3PhcEBucWO{b4Pjc5Bq[yCjbnHsfZNqew>? NGTiZ3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{ixNFU6OSd-Mke4NVA2QTF:L3G+
NIH/3T3 NEjBT4tHfW6ldHnvckBie3OjeR?= MlT0TY5pcWKrdHnvckBw\iCqZXTn[Yhw\yC|aXfuZYxqdmdicHH0bJdigSCrbjDtc5V{\SCQSVivN3Q{KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gbIVl\2Wqb3etbY5lfWOnZDDTcY8uTUeIUDDjbYxq[XK7IITyZY5{dG:lYYTpc44h[nliRFHQTUB{fGGrbnnu[{Bj[XOnZDDjc45nd2OjbDDtbYNzd3Olb4DpZ{BidmGueYPpdy=> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzhzMEW5NUc,Ojd6MUC1PVE9N2F-
MG 63 (6-TG R) MmXldWhVWyCjc4PhfS=> MVPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDNS{A3OyBqNj3US{BTMSClZXzsdy=> M13abVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41 NYTrfnBIeUiWUzDhd5NigQ>? NXH5e3hJeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>? M{D3b|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
U-2 OS NHzwU3FyUFSVIHHzd4F6 MorWdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWU0zKE:VIHPlcIx{ NH\KdVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
A673 MXjxTHRUKGG|c3H5 M33ISpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| M{LtfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-12 NFXTPHNyUFSVIHHzd4F6 NIDlOYRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStNVIh[2WubIO= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) NGrrVZpyUFSVIHHzd4F6 MYDxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? MlvlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1 NYjs[XhxeUiWUzDhd5NigQ>? NGHRZmVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> NXHVZXkyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 NIfGeFVyUFSVIHHzd4F6 MXrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| MmTtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 NXf6OJczeUiWUzDhd5NigQ>? NHXTdoRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU3Hvd{0zKGOnbHzz NELvS5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 MXfxTHRUKGG|c3H5 NHjyeZJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=> MkLaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC MXXxTHRUKGG|c3H5 Mmf1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH MXvxTHRUKGG|c3H5 NYXP[|lFeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM> NITrbno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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

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

Solubility (25°C)

In vitro

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

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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