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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Cited by 12 Publications

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.
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 Ml7HR5l1d3irY3n0fUBie3OjeR?= M{n0b54yOCEQvF2= MmfuTWM2OD1zMjFOwG0> NIHK[lEzOjV3M{O1OS=>
A2780cp20 MULDfZRwgGmlaYT5JIF{e2G7 NHrFU3V,OTBizszN MkiwTWM2OD15LkWg{txO MYWyNlU2OzN3NR?=
SKOV3ip1 MWfDfZRwgGmlaYT5JIF{e2G7 Mny0glExKM7:TR?= Mmm4TWM2OD1{NDFOwG0> NVLzfYhxOjJ3NUOzOVU>
SKOV3TRip2 MV3DfZRwgGmlaYT5JIF{e2G7 MoDoglExKM7:TR?= MnSzTWM2OD1zMjFOwG0> MoniNlI2PTN|NUW=
HeyA8 NE\VZ|lEgXSxeHnjbZR6KGG|c3H5 MVv+NVAh|ryP NYXyW4RoUUN3ME2xPEDPxE1? M1rLdFIzPTV|M{W1
HeyA8MDR NUD0fIw6S3m2b4jpZ4l1gSCjc4PhfS=> M2jNb54yOCEQvF2= NXK0PJhMUUN3ME24JO69VQ>? MnHkNlI2PTN|NUW=
OS5 M2HRNmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MV7+OUDPxE1? NGe3[Hpz\WS3Y3XzJJRp\SCycn;sbYZmemG2aX;u M37mWFI{OjR|NUm1
OS18 MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGr6dol,PSEQvF2= NIDKb5Bz\WS3Y3XzJJRp\SCycn;sbYZmemG2aX;u NH2xRVczOzJ2M{W5OS=>
Glioblastoma initiating cells MlzKR5l1d3irY3n0fUBie3OjeR?= MYL+NVAh|ryP M2HWZWlvcGmkaYTzJGNmdGxiVnnhZoltcXS7 MljiNlM1QDJ4N{G=
Glioblastoma initiating cells MVvGeY5kfGmxbjDhd5NigQ>? NHSwNZp,OTBizszN MULpcohq[mm2czDu[ZVzd3OyaHXy[UBnd3KvYYTpc44> MWKyN|Q5OjZ5MR?=
Glioblastoma initiating cells MmTuR5l1d3irY3n0fUBie3OjeR?= NHHMTIh,OTBizszN NX6wTVk4cW6mdXPld{BieG:ydH;zbZM> M2HXSVI{PDh{Nkex
Glioblastoma initiating cells NEfXd4FHfW6ldHnvckBie3OjeR?= NXXNWmt2hjFyIN88US=> NGLRdZpld3ewcnXneYxifGW|IITo[UBUUEhic3nncoFtcW6pIIDheIh4[Xl? NFTBcnQzOzR6Mk[3NS=>
Glioblastoma initiating cells MV;GeY5kfGmxbjDhd5NigQ>? MoPZglExKM7:TR?= M2LJdWlvcGmkaYTzJJRp\SCHeIDy[ZN{cW:wIH;mJGdmdmW|IFnueo9tfmWmIHnuJG1icW62YXnubY5oKFCudYLpdI91\W6leR?= M3zSR|I{PDh{Nkex
Glioblastoma initiating cells M4LZUWZ2dmO2aX;uJIF{e2G7 MUT+NVAh|ryP NFf4fXFKdmirYnn0d{BOd3SrbHn0fUwhUW64YYPpc44tKGGwZDDNbYdz[XSrb36= MmXuNlM1QDJ4N{G=
LOX IMVI M2TqT2Z2dmO2aX;uJIF{e2G7 M1fHNFExKM7:TR?= MVHEUXNQ NW\FUlI5cW6qaXLpeJMhUGWmZ3Xoc4cuT0yLIIDheIh4[Xl? MlP2NlM6OzV7MkW=
UACC 257 M2nkUWZ2dmO2aX;uJIF{e2G7 Ml;GNVAh|ryP M17TRWROW09? M3facYlvcGmkaYTzJGhm\GenaH;nMWdNUSCyYYToe4F6 NIDmXJMzOzl|NUmyOS=>
LOX IMVI MnH0SpVv[3Srb36gZZN{[Xl? MXixNEDPxE1? Mo[1SG1UVw>? MUnpcoR2[2W|IFexJINmdGxiY4njcIUh[XK{ZYP0 MWOyN|k{PTl{NR?=
UACC 257 M3r2OWZ2dmO2aX;uJIF{e2G7 NFHVdHoyOCEQvF2= NUOwW|BQTE2VTx?= MmD4bY5lfWOnczDHNUBk\WyuIHP5Z4xmKGG{cnXzeC=> Mn3nNlM6OzV7MkW=
LOX IMVI M3;adGN6fG:6aXPpeJkh[XO|YYm= NFnSd2wyOCEQvF2= MYPEUXNQ Mmf4[IVkemWjc3XzJJR2dW:{IHPlcIwhfmmjYnnsbZR6 M3zBWlI{QTN3OUK1
UACC 257 M4n6VWN6fG:6aXPpeJkh[XO|YYm= MkjpNVAh|ryP MWLEUXNQ M1LGR4Rm[3KnYYPld{B1fW2xcjDj[YxtKH[rYXLpcIl1gQ>? MlPyNlM6OzV7MkW=
LOX IMVI MUfBdI9xfG:|aYOgZZN{[Xl? NYjMUIV{OTBizszN NEDP[JhFVVOR NEHY[3lqdmS3Y3XzJIFxd3C2b4Ppdy=> Ml\2NlM6OzV7MkW=
UACC 257 NIPieFhCeG:ydH;zbZMh[XO|YYm= MYqxNEDPxE1? M2ntZWROW09? MWHpcoR2[2W|IHHwc5B1d3Orcx?= MXKyN|k{PTl{NR?=
ACHN MnvzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVi0VoNphjVizszN M{mwfGROW09? M3S4[2lEPTB;Mj2z5qCK|ryP NVWwenZuOjVyOUO0PVE>
769-P Ml7QS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVPwT2NkhjVizszN M3PmdGROW09? NWLRUHVNUUN3ME2yMVPjiIoQvF2= M1zyNlI2ODl|NEmx
786-O M1\MUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXfY[3BPhjVizszN NYjRdXNoTE2VTx?= NXPiS|BGUUN3ME2yMVPjiIoQvF2= M3m2PFI2ODl|NEmx
786-O SuR Mn\OS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHHGOJZ,PSEQvF2= NVfW[Wd4TE2VTx?= MVLJR|UxRTJvM,MAje69VQ>? MXyyOVA6OzR7MR?=
SP53 MoTtSpVv[3Srb36gZZN{[Xl? NXvBR|NFOzBizszN MYrEUXNQ NGPaOGNqdmirYnn0d{Bk\WyuIHHkbIV{cW:wIHHu[EBucWe{YYTpc44> NI\WR|EzPjh6NU[wPC=>
SP53 M{fnO2Z2dmO2aX;uJIF{e2G7 NWm2U3UyOzBizszN Mm\pSG1UVw>? M1L0fIlvcGmkaYTzJJRp\SCYTFG0MY1m\GmjdHXkJGZCUyC|aXfuZYxqdmdicHH0bJdigQ>? MlPnNlY5QDV4MEi=
HS5 M2Xu[2Z2dmO2aX;uJIF{e2G7 NHLyWlk{OCEQvF2= M2TQbGROW09? NYmxeZVIcW6qaXLpeJMh[2WubDDh[Ihme2mxbjDhcoQhdWmpcnH0bY9v NG\DZngzPjh6NU[wPC=>
HS27a NWXmPGprTnWwY4Tpc44h[XO|YYm= NU[zOIpKOzBizszN NUHu[IZZTE2VTx?= MlTYbY5pcWKrdIOgZ4VtdCCjZHjld4lwdiCjbnSgcYloemG2aX;u Mmf3NlY5QDV4MEi=
SP53 M2TK[WN6fG:6aXPpeJkh[XO|YYm= NWSwb5R3OzBizszN NHvyO41FVVOR Mnm3bY5lfWOnczDheZRweGijZ4m= NEHIbpozPjh6NU[wPC=>
Jeko NGfwWWdEgXSxeHnjbZR6KGG|c3H5 MUSzNEDPxE1? MVjEUXNQ Mo\kbY5lfWOnczDheZRweGijZ4m= NGPFdZAzPjh6NU[wPC=>

... 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]

Protocol

Cell Research:

[1]

+ 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:

[1]

+ 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.
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

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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
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
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
NCT02195973 Completed Recurrent Ovarian Cancer University of Alabama at Birmingham|Novartis Pharmaceuticals September 2014 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID