Sonidegib (Erismodegib, NVP-LDE225)

Catalog No.S2151

Sonidegib (Erismodegib, NVP-LDE225) Chemical Structure

Molecular Weight(MW): 485.5

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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In DMSO USD 210 In stock
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3 Customer Reviews

  • RU-SKI 43 blocks Shh signaling. (a) RU-SKI 43 blocks Gli activation. NIH 3T3 cells were cotransfected with vectors encoding 8× Gli-binding site (GliBS)-Firefly luciferase (unless indicated otherwise), Renilla luciferase reporter (pRL-TK) and Shh. Confluent cells were treated with DMSO, 10 μM LDE225, 10 μM RU-SKI 43 or 10 μM C-2. The firefly luciferase (FL)/Renilla luciferase (RL) ratio in cell lysates was calculated and normalized to that measured in DMSO-treated samples; error bars represent mean ± s.d. (n = 2–3). 

    Nat Chem Biol 2013 9, 247-9. Sonidegib (Erismodegib, NVP-LDE225) purchased from Selleck.

    Western blot analysis on total cell lysates from renal cancer cell lines treated with NVP-LDE225 at different concentrations. Densitometric measurements were normalised to b-actin and reported under western blot images.

    Br J Cancer 2014 111(6), 1168-79. Sonidegib (Erismodegib, NVP-LDE225) purchased from Selleck.

  • NVP-LDE225, everolimus, sunitinib, and their combination interfere with actin and with intracellular organisation of focal adhesion points. Cytoskeleton organisation of 786-O SuR treated with NVP-LDE225 ( 2.5 uM ), everolimus (1 uM ), sunitinib (1 uM ), and their combination for 24 h was analysed by confocal microscopy. Actin-based structures were revealed by rhodaminated phalloidin staining (red fluorescence). Localisation of focal adhesion points was obtained by immunofluorescent staining of p-paxillin (green fluorescence). Merged row images show overlapping of p-paxillin and actin signals. Moreover, all captures were shown in transmitted light. Scale bars, 10 um.

    Br J Cancer 2014 111(6), 1168-79. Sonidegib (Erismodegib, NVP-LDE225) purchased from Selleck.

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.
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 Mn61R5l1d3irY3n0fUBie3OjeR?= M2TtRZ4yOCEQvF2= MkHnTWM2OD1zMjFOwG0> NV7COWlEOjJ3NUOzOVU>
A2780cp20 NXjH[nBTS3m2b4jpZ4l1gSCjc4PhfS=> M3z2VZ4yOCEQvF2= MkTtTWM2OD15LkWg{txO NWDsU49vOjJ3NUOzOVU>
SKOV3TRip2 NWHMZnJmS3m2b4jpZ4l1gSCjc4PhfS=> MXX+NVAh|ryP NXyxWmE4UUN3ME2xNkDPxE1? M2TWdFIzPTV|M{W1
HeyA8MDR Ml;aR5l1d3irY3n0fUBie3OjeR?= Ml:wglExKM7:TR?= MWXJR|UxRThizszN MX6yNlU2OzN3NR?=
OS5 NVrRVXdkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXSwOpV1hjVizszN MljXdoVlfWOnczD0bIUheHKxbHnm[ZJifGmxbh?= NYPZUlZCOjN{NEO1PVU>
OS18 MmjRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIjVdJJ,PSEQvF2= MnvtdoVlfWOnczD0bIUheHKxbHnm[ZJifGmxbh?= MV:yN|I1OzV7NR?=
Glioblastoma initiating cells NEOwSFVEgXSxeHnjbZR6KGG|c3H5 NVvC[3lDhjFyIN88US=> MWPJcohq[mm2czDD[YxtKF[rYXLpcIl1gQ>? MnvwNlM1QDJ4N{G=
Glioblastoma initiating cells NGf4TY9HfW6ldHnvckBie3OjeR?= NVzleWFGhjFyIN88US=> NFPsNGpqdmirYnn0d{Bv\XW{b4PwbIVz\SCob4LtZZRqd25? NHv0NXUzOzR6Mk[3NS=>
Glioblastoma initiating cells M335VWN6fG:6aXPpeJkh[XO|YYm= M2PyN54yOCEQvF2= MmLEbY5lfWOnczDhdI9xfG:|aYO= NXzXdXI3OjN2OEK2O|E>
Glioblastoma initiating cells M2rYWGZ2dmO2aX;uJIF{e2G7 NYrFTWJohjFyIN88US=> NFTFUmlld3ewcnXneYxifGW|IITo[UBUUEhic3nncoFtcW6pIIDheIh4[Xl? M4rzWlI{PDh{Nkex
Glioblastoma initiating cells M3nIOGZ2dmO2aX;uJIF{e2G7 M12ybp4yOCEQvF2= NVTPdY5QUW6qaXLpeJMhfGinIFX4dJJme3Orb36gc4YhT2WwZYOgTY53d2y4ZXSgbY4hVWGrboThbY5qdmdiUHz1dolxd3SnbnP5 NEDTZWUzOzR6Mk[3NS=>
Glioblastoma initiating cells NUe1bWRZTnWwY4Tpc44h[XO|YYm= MV3+NVAh|ryP MojlTY5pcWKrdIOgUY91cWyrdImsJGlvfmG|aX;uMEBidmRiTXnndoF1cW:w MVSyN|Q5OjZ5MR?=
LOX IMVI NXXX[3hkTnWwY4Tpc44h[XO|YYm= M{LjVVExKM7:TR?= MX;EUXNQ NIT4V|JqdmirYnn0d{BJ\WSpZXjv[{1IVElicHH0bJdigQ>? MVOyN|k{PTl{NR?=
UACC 257 NInrTGJHfW6ldHnvckBie3OjeR?= MlnONVAh|ryP MYHEUXNQ NHjHdVZqdmirYnn0d{BJ\WSpZXjv[{1IVElicHH0bJdigQ>? NEjITY4zOzl|NUmyOS=>
LOX IMVI NEj6UW5HfW6ldHnvckBie3OjeR?= MkXmNVAh|ryP NUG2W4p7TE2VTx?= NIPiTndqdmS3Y3XzJGcyKGOnbHygZ5lkdGViYYLy[ZN1 NE\BRVQzOzl|NUmyOS=>
UACC 257 M1TQ[mZ2dmO2aX;uJIF{e2G7 MX:xNEDPxE1? NFzzeXJFVVOR M3;vOIlv\HWlZYOgS|Eh[2WubDDjfYNt\SCjcoLld5Q> MWqyN|k{PTl{NR?=
UACC 257 M2H2VWN6fG:6aXPpeJkh[XO|YYm= MVqxNEDPxE1? NFfBO4hFVVOR NHzvRVFl\WO{ZXHz[ZMhfHWvb4KgZ4VtdCC4aXHibYxqfHl? NULs[XhsOjN7M{W5NlU>
UACC 257 NHLrZVRCeG:ydH;zbZMh[XO|YYm= MYmxNEDPxE1? NUnwO5FlTE2VTx?= MWXpcoR2[2W|IHHwc5B1d3Orcx?= NEmzTHMzOzl|NUmyOS=>
ACHN NIrJcllIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEPLd5Z,PSEQvF2= Mli5SG1UVw>? NXzMepZHUUN3ME2yMVPjiIoQvF2= M{XLeVI2ODl|NEmx
769-P M2DyTGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2C1bJ42KM7:TR?= NWLSXFdDTE2VTx?= NXPEbW04UUN3ME2yMVPjiIoQvF2= NUPYUoxkOjVyOUO0PVE>
786-O NWezR5poT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NG\XNoJ,PSEQvF2= NUjoUG5RTE2VTx?= M1nwNGlEPTB;Mj2z5qCK|ryP MUWyOVA6OzR7MR?=
786-O SuR NHXPW5JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3fjb542KM7:TR?= Ml;iSG1UVw>? MYnJR|UxRTJvM,MAje69VQ>? NX:4WG9QOjVyOUO0PVE>
SP53 NX\ZPVFUTnWwY4Tpc44h[XO|YYm= MXWzNEDPxE1? M4fKXmROW09? NXjIfHhQcW6qaXLpeJMh[2WubDDh[Ihme2mxbjDhcoQhdWmpcnH0bY9v M33HN|I3QDh3NkC4
HS5 M2O5fGZ2dmO2aX;uJIF{e2G7 Mlq1N|Ah|ryP NVyyN3lJTE2VTx?= MlvtbY5pcWKrdIOgZ4VtdCCjZHjld4lwdiCjbnSgcYloemG2aX;u NVvQPZRwOjZ6OEW2NFg>
HS27a MYPGeY5kfGmxbjDhd5NigQ>? NWLZPYJVOzBizszN MYjEUXNQ M37JTIlvcGmkaYTzJINmdGxiYXTo[ZNqd25iYX7kJI1q\3KjdHnvci=> Mn;mNlY5QDV4MEi=
SP53 M3HJVWN6fG:6aXPpeJkh[XO|YYm= M4HrTlMxKM7:TR?= NV7XT3h2TE2VTx?= MXTpcoR2[2W|IHH1eI9xcGGpeR?= MWeyOlg5PTZyOB?=
Jeko NV7FT2N4S3m2b4jpZ4l1gSCjc4PhfS=> NXv0W41GOzBizszN M4C2TWROW09? MlO1bY5lfWOnczDheZRweGijZ4m= MWSyOlg5PTZyOB?=

... Click to View More Cell Line Experimental Data

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]


Cell Research:


+ Expand
  • 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:


+ Expand
  • Animal Models: Orthotopic Ptch+/-p53-/- medulloblastoma allograft model in athymic nude mice
  • Formulation: 0.5% sodium carboxymethyl cellulose
  • 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.

* 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


CAS No. 956697-53-3
Storage powder
in solvent

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02254551 Terminated Multiple Myeloma SCRI Development Innovations LLC|Novartis January 2015 Phase 2
NCT02138929 Active not recruiting Esophageal Cancer M.D. Anderson Cancer Center|Novartis|National Cancer Institute (NCI) November 10 2014 Phase 1
NCT02195973 Completed Recurrent Ovarian Cancer University of Alabama at Birmingham|Novartis Pharmaceuticals September 2014 Phase 1
NCT02182622 Unknown status Prostate Cancer Martin Gutierrez|Novartis|Hackensack Meridian Health July 2014 Phase 1
NCT02151864 Active not recruiting Hepatocellular Carcinoma|Cirrhosis Jason K. Sicklick M.D.|Novartis Pharmaceuticals|University of California San Diego July 2014 Phase 1
NCT02027376 Unknown status Advanced Breast Cancer Spanish Breast Cancer Research Group|Novartis May 2014 Phase 1

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Hedgehog/Smoothened Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID