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Sonidegib (NVP-LDE225)

For research use only.

Catalog No.S2151 Synonyms: Erismodegib

43 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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10mM (1mL in DMSO) GBP 171 In stock
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GBP 384 In stock
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Selleck's Sonidegib (NVP-LDE225) has been cited by 43 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 MVrDfZRwgGmlaYT5JIF{e2G7 Mlj1glExKM7:TR?= NImyRYxKSzVyPUGyJO69VQ>? M13TWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUWzN|U2Lz5{MkW1N|M2PTxxYU6=
A2780cp20 M{DENmN6fG:6aXPpeJkh[XO|YYm= NVLWcXVMhjFyIN88US=> M2rDfWlEPTB;Nz61JO69VQ>? M{HNc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUWzN|U2Lz5{MkW1N|M2PTxxYU6=
SKOV3ip1 MVPDfZRwgGmlaYT5JIF{e2G7 M2jrTp4yOCEQvF2= M4XZc2lEPTB;MkSg{txO NGTrRmg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW1N|M2PSd-MkK1OVM{PTV:L3G+
SKOV3TRip2 MlH2R5l1d3irY3n0fUBie3OjeR?= NVjGSZBjhjFyIN88US=> MVHJR|UxRTF{IN88US=> NEjKWJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW1N|M2PSd-MkK1OVM{PTV:L3G+
HeyA8 NVvKZZNiS3m2b4jpZ4l1gSCjc4PhfS=> NFraNIJ,OTBizszN M2LtTmlEPTB;MUig{txO MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV3M{O1OUc,OjJ3NUOzOVU9N2F-
HeyA8MDR MoC5R5l1d3irY3n0fUBie3OjeR?= NWf2WldihjFyIN88US=> MWHJR|UxRThizszN MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV3M{O1OUc,OjJ3NUOzOVU9N2F-
OS5 MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUj+OUDPxE1? NU\vSZZMemWmdXPld{B1cGVicILvcIln\XKjdHnvci=> NU\RW3RLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyOFM2QTVpPkKzNlQ{PTl3PD;hQi=>
OS18 NXT3RVVLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NF;h[49,PSEQvF2= MXjy[YR2[2W|IITo[UBxem:uaX\ldoF1cW:w NVe1cohwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyOFM2QTVpPkKzNlQ{PTl3PD;hQi=>
Glioblastoma initiating cells NHXycmlEgXSxeHnjbZR6KGG|c3H5 NFjBVIR,OTBizszN M3jjbWlvcGmkaYTzJGNmdGxiVnnhZoltcXS7 MlvBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OEK2O|EoRjJ|NEiyOlcyRC:jPh?=
Glioblastoma initiating cells NXzuSGJoTnWwY4Tpc44h[XO|YYm= MonYglExKM7:TR?= MV\pcohq[mm2czDu[ZVzd3OyaHXy[UBnd3KvYYTpc44> Mn7zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OEK2O|EoRjJ|NEiyOlcyRC:jPh?=
Glioblastoma initiating cells NFrLXm9EgXSxeHnjbZR6KGG|c3H5 Mn:zglExKM7:TR?= MnLabY5lfWOnczDhdI9xfG:|aYO= MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR6Mk[3NUc,OjN2OEK2O|E9N2F-
Glioblastoma initiating cells M2HXfGZ2dmO2aX;uJIF{e2G7 NF3XVYN,OTBizszN MnzD[I94dnKnZ4XsZZRmeyC2aHWgV2hJKHOrZ37hcIlv\yCyYYToe4F6 NVq0[W5KRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0PFI3PzFpPkKzOFgzPjdzPD;hQi=>
Glioblastoma initiating cells NGnROGJHfW6ldHnvckBie3OjeR?= MkK4glExKM7:TR?= MkSxTY5pcWKrdIOgeIhmKEW6cILld5Nqd25ib3[gS4Vv\XNiSX72c4x3\WRiaX6gUYFqdnSjaX7pcochWGy3cnnwc5RmdmO7 M2XmTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEiyOlcyLz5{M{S4NlY4OTxxYU6=
Glioblastoma initiating cells M1vLT2Z2dmO2aX;uJIF{e2G7 NYLzZm5EhjFyIN88US=> NUewPFVGUW6qaXLpeJMhVW:2aXzpeJktKEmwdnHzbY9vNCCjbnSgUYloemG2aX;u NIf3R5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S4NlY4OSd-MkO0PFI3PzF:L3G+
LOX IMVI MnuwSpVv[3Srb36gZZN{[Xl? MlG2NVAh|ryP NHvKXndFVVOR M3r5[olvcGmkaYTzJGhm\GenaH;nMWdNUSCyYYToe4F6 MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl|NUmyOUc,OjN7M{W5NlU9N2F-
UACC 257 MWfGeY5kfGmxbjDhd5NigQ>? MUOxNEDPxE1? M{C3dGROW09? Ml3DbY5pcWKrdIOgTIVl\2Wqb3etS2xKKHCjdHj3ZZk> MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl|NUmyOUc,OjN7M{W5NlU9N2F-
LOX IMVI NYTZRWhYTnWwY4Tpc44h[XO|YYm= Mn\xNVAh|ryP NX\r[mZDTE2VTx?= M2\yeYlv\HWlZYOgS|Eh[2WubDDjfYNt\SCjcoLld5Q> NXP2OW1[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|U6OjVpPkKzPVM2QTJ3PD;hQi=>
UACC 257 M2nLXWZ2dmO2aX;uJIF{e2G7 NXn5[XJSOTBizszN MXXEUXNQ M4P4Uolv\HWlZYOgS|Eh[2WubDDjfYNt\SCjcoLld5Q> MnrsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ|OUO1PVI2RC:jPh?=
LOX IMVI NV70Z|ZPS3m2b4jpZ4l1gSCjc4PhfS=> M3r0d|ExKM7:TR?= MnrBSG1UVw>? MnPq[IVkemWjc3XzJJR2dW:{IHPlcIwhfmmjYnnsbZR6 NWrscpZIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|U6OjVpPkKzPVM2QTJ3PD;hQi=>
UACC 257 M2DzWWN6fG:6aXPpeJkh[XO|YYm= MYixNEDPxE1? MlTWSG1UVw>? MWLk[YNz\WG|ZYOgeJVud3JiY3XscEB3cWGkaXzpeJk> NVz0WGxqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|U6OjVpPkKzPVM2QTJ3PD;hQi=>
LOX IMVI MknwRZBweHSxc3nzJIF{e2G7 M17Gb|ExKM7:TR?= NHHzPJlFVVOR M3XVTolv\HWlZYOgZZBweHSxc3nz MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl|NUmyOUc,OjN7M{W5NlU9N2F-
UACC 257 MnXjRZBweHSxc3nzJIF{e2G7 NWLrPXQ{OTBizszN NUHMd|JGTE2VTx?= NWTBXIJOcW6mdXPld{BieG:ydH;zbZM> NUDZOllDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|U6OjVpPkKzPVM2QTJ3PD;hQi=>
ACHN M{XsNWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX;Ob2xXhjVizszN NHPMOm9FVVOR NF\xcVNKSzVyPUKtN-KBkc7:TR?= NWXKb3lLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPVM1QTFpPkK1NFk{PDlzPD;hQi=>
769-P NYnJUm1nT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYn+OUDPxE1? MmPiSG1UVw>? M2fYVGlEPTB;Mj2z5qCK|ryP M1yxZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEmzOFkyLz5{NUC5N|Q6OTxxYU6=
786-O MmXIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX3mbVBWhjVizszN NYjnXmhzTE2VTx?= NV7EdldMUUN3ME2yMVPjiIoQvF2= NYfOcnYxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPVM1QTFpPkK1NFk{PDlzPD;hQi=>
786-O SuR M4m0UGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHjTT3J,PSEQvF2= NGTTV49FVVOR NFvFb5pKSzVyPUKtN-KBkc7:TR?= M4XtTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEmzOFkyLz5{NUC5N|Q6OTxxYU6=
SP53 NIXod2FHfW6ldHnvckBie3OjeR?= M3rOelMxKM7:TR?= NUD3ZVF4TE2VTx?= MmPObY5pcWKrdIOgZ4VtdCCjZHjld4lwdiCjbnSgcYloemG2aX;u NIj3NZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki4OVYxQCd-Mk[4PFU3ODh:L3G+
SP53 MUnGeY5kfGmxbjDhd5NigQ>? NHTnSJk{OCEQvF2= MorMSG1UVw>? MontbY5pcWKrdIOgeIhmKF[OQUStcYVlcWG2ZXSgSmFMKHOrZ37hcIlv\yCyYYToe4F6 MkXrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6OEW2NFgoRjJ4OEi1OlA5RC:jPh?=
HS5 NVTH[mN4TnWwY4Tpc44h[XO|YYm= M1jIR|MxKM7:TR?= M1zBcGROW09? NFfNU|hqdmirYnn0d{Bk\WyuIHHkbIV{cW:wIHHu[EBucWe{YYTpc44> NFXWR3E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki4OVYxQCd-Mk[4PFU3ODh:L3G+
HS27a M4H3XmZ2dmO2aX;uJIF{e2G7 MWqzNEDPxE1? NWPjfplGTE2VTx?= MmCwbY5pcWKrdIOgZ4VtdCCjZHjld4lwdiCjbnSgcYloemG2aX;u NXnhc5VsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4PFU3ODhpPkK2PFg2PjB6PD;hQi=>
SP53 NXfrUJNDS3m2b4jpZ4l1gSCjc4PhfS=> NU\RbYY2OzBizszN M1HXbmROW09? M4XRNolv\HWlZYOgZZV1d3CqYXf5 MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh6NU[wPEc,OjZ6OEW2NFg9N2F-
Jeko NVnkRnhyS3m2b4jpZ4l1gSCjc4PhfS=> NFXPd2g{OCEQvF2= NYnJc5BPTE2VTx?= NUH0RYQ4cW6mdXPld{BifXSxcHjh[5k> MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh6NU[wPEc,OjZ6OEW2NFg9N2F-
U2OS NFHhWItHfW6ldHnvckBie3OjeR?= NFjJWZAzKGi{cx?= NWfsbXduTGm|cHzhZ4Vu\W62IH;mJHs{UF2leXPsc5BidWmwZTDmdo9uKHerbHSgeJlx\SCVbX:g[ZhxemW|c3XkJIlvKFV{T2OgZ4VtdHNiYX\0[ZIhOiCqcoOgZpkhe2OrboTpcIxifGmxbjDjc5VvfGmwZzygT4khRSByLkCwOkDPxE1w Ml;2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyNkO1NlIoRjJ|ME[zOVIzRC:jPh?=
NIH/3T3 NH7hfZNHfW6ldHnvckBie3OjeR?= NWXjeIoxUW6qaXLpeIlwdiCxZjDo[YRo\WixZzDzbYdv[WyrbnegdIF1cHejeTDpckBud3W|ZTDOTWgwO1R|IHPlcIx{KGW6cILld5Nqdmdid3ns[EB1gXCnIGPtc{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gS4xqKG2UTlGg[ZhxemW|c3nvckBjgSCUVD3QR3IhdWW2aH;kMEBKSzVyIE2gNE4xODR2IN88UU4> MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzhzMEW5NUc,Ojd6MUC1PVE9N2F-
NIH/3T3 MYjGeY5kfGmxbjDhd5NigQ>? MmfMTY5pcWKrdHnvckBw\iCqZXTn[Yhw\yC|aXfuZYxqdmdicHH0bJdigSCrbjDtc5V{\SCQSVivN3Q{KGOnbHzzJIhiemKxcnnu[{BUdW9iRES3O2ghdXW2YX70JIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDHcIkhdVKQQTDlfJBz\XO|aX;uJIJ6KFKWLWDDVkBu\XSqb3SsJGlEPTBiPTCwMlAzOjdizszNMi=> MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzhzMEW5NUc,Ojd6MUC1PVE9N2F-
NIH/3T3 NH7vd|FHfW6ldHnvckBie3OjeR?= NInabIYzPCCqcoO= NGLkWGRKdmirYnn0bY9vKG:oIHjl[IdmcG:pIIPp[45idGmwZzDwZZRpf2G7IHnuJI1wfXOnIF7JTE8{XDNiY3XscJMhdWWjc4Xy[YQh[W[2ZYKgNlQhcHK|IHL5JGdtcS2mdXHsJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiSVO1NEA:KDBwMEC2JO69VS5? NFvUeWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{ixNFU6OSd-Mke4NVA2QTF:L3G+
TM3 MlfFSpVv[3Srb36gZZN{[Xl? MVW0PEBpenN? MmXBTY5pcWKrdHnvckBw\iCKaDDzbYdv[WyrbnegdIF1cHejeTDpckBud3W|ZTDUUVMh[2WubIOgZZN{\XO|ZXSgZZMh\G:5boLl[5Vt[XSrb36gc4YhT2yrMTDn[Y5mKGW6cILld5Nqd25iYX\0[ZIhPDhiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OCB;IECuNFAyOiEQvF2u NWjkepVDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5O|YzOTVpPkK2PVc3OjF3PD;hQi=>
NIH3T3 NILOc2NHfW6ldHnvckBie3OjeR?= MUe0PEBpenN? MmfTTY5pcWKrdHnvckBw\iCVSFigd4lodmGuaX7nJJBifGi5YYmgbY4hdW:3c3WgUmlJO1R|IHPlcIx{KG2nYYP1doVlKGGodHXyJFQ5KGi{czDifUBIdGlvbIXjbYZmemG|ZTDy[ZBwenSncjDhd5NigSxiSVO1NEA:KDBwMEC1OUDPxE1w MmfUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzN{[zPVYoRjJ2MUe2N|k3RC:jPh?=
NIH3T3 MYXGeY5kfGmxbjDhd5NigQ>? M17nS|Q5KGi{cx?= NWjwSYY4UW6qaXLpeIlwdiCxZjDTc45q[y2rbnT1Z4VlKGinZHflbI9oKHOrZ37hcIxqdmdiaX6gcY92e2ViTlnIN3Q{KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDHcIkudHWlaX\ldoF{\SC{ZYDvdpRmeiCjc4PhfUwhUUN3MDC9JFAvODB3NTFOwG0v M2jMXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OEKwOVU1Lz5{NkiyNFU2PDxxYU6=
NIH/3T3 MonrSpVv[3Srb36gZZN{[Xl? NGCxcm5KdmirYnn0bY9vKG:oIHjl[IdmcG:pIIPp[45idGmwZzDwZZRpf2G7IHX4dJJme3OnZDDpckBud3W|ZTDOTWgwO1R|IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhcGWmZ3Xoc4cucW6mdXPl[EBIdGlvMjDhZ4N2dXWuYYTpc44h[XRidHnwJI9nKHC{aX3hdpkh[2muaXGgZpkhTEGSSTDzeIFqdmmwZzDiZZNm\CClb37mc4NidCCvaXPyc5Nkd3CrYzDhcoFtgXOrcx?= MkH1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd6MUC1PVEoRjJ5OEGwOVkyRC:jPh?=
NIH/3T3 M{PxNGZ2dmO2aX;uJIF{e2G7 MWTJcohq[mm2aX;uJI9nKGinZHflbI9oKHOrZ37hcIlv\yCyYYToe4F6KGmwIH3veZNmKE6LSD:zWFMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDo[YRo\WixZz3pcoR2[2WmIGPtc{1GT0[SIHPpcIlienlidILhcpNtd2OjdHnvckBjgSCGQWDJJJN1[WmwaX7nJIJie2WmIHPvcoZw[2GuIH3pZ5Jwe2OxcHnjJIFv[Wy7c3nz NXzsWFBPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke4NVA2QTFpPkK3PFExPTlzPD;hQi=>
MG 63 (6-TG R) MVzxTHRUKGG|c3H5 NFS1WFhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBOTyB4MzCoOk1VTyCUKTDj[Yxtew>? NIrMW5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 MmrodWhVWyCjc4PhfS=> MnjSdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVog1OSClZXzsdy=> Ml7xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
U-2 OS MkPIdWhVWyCjc4PhfS=> M3jPU5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHUuOiCRUzDj[Yxtew>? NWn1bmxIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673 M1n6NpFJXFNiYYPzZZk> MmDXdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN? MmL4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-12 M4jiTJFJXFNiYYPzZZk> MljJdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| MmrSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R) NF7QUGZyUFSVIHHzd4F6 MkDVdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy| Mm\TQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1 NWr4U2xReUiWUzDhd5NigQ>? MX3xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= NWnBR3FMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 NHXkbXRyUFSVIHHzd4F6 MWnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| NUTNSnZCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 NFzwbmhyUFSVIHHzd4F6 NWPseIh1eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPhc5MuOiClZXzsdy=> NFnx[mo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 MkKwdWhVWyCjc4PhfS=> M2j5UZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz MnLwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC Mn\kdWhVWyCjc4PhfS=> NVjpOI5beUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> M1jH[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-SH MVPxTHRUKGG|c3H5 MYfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?= M3\nNVxiKHSjcnfleF0oZ2KuYX7rK{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
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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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID