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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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 MYXDfZRwgGmlaYT5JIF{e2G7 M2HCUp4yOCEQvF2= NGrUN4xKSzVyPUGyJO69VQ>? M4n5[FIzPTV|M{W1
A2780cp20 NWXHdHBzS3m2b4jpZ4l1gSCjc4PhfS=> MlO5glExKM7:TR?= M3;rZmlEPTB;Nz61JO69VQ>? NHjZRYczOjV3M{O1OS=>
SKOV3ip1 MYTDfZRwgGmlaYT5JIF{e2G7 NYfM[HlEhjFyIN88US=> MlHuTWM2OD1{NDFOwG0> NEXYeoozOjV3M{O1OS=>
SKOV3TRip2 NUHROpl5S3m2b4jpZ4l1gSCjc4PhfS=> MmTaglExKM7:TR?= NIfLVI1KSzVyPUGyJO69VQ>? NUjpO|F2OjJ3NUOzOVU>
HeyA8 Mn7iR5l1d3irY3n0fUBie3OjeR?= NFTDTlB,OTBizszN MX\JR|UxRTF6IN88US=> M3ntT|IzPTV|M{W1
HeyA8MDR M2jjPWN6fG:6aXPpeJkh[XO|YYm= M4jEOZ4yOCEQvF2= M1PMOWlEPTB;ODFOwG0> MlfxNlI2PTN|NUW=
OS5 MmTBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGTN[mV,PSEQvF2= MlSxdoVlfWOnczD0bIUheHKxbHnm[ZJifGmxbh?= NF3mV2gzOzJ2M{W5OS=>
OS18 NXjIcllTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NX;CelJNhjVizszN NFflfldz\WS3Y3XzJJRp\SCycn;sbYZmemG2aX;u MXOyN|I1OzV7NR?=
Glioblastoma initiating cells MVHDfZRwgGmlaYT5JIF{e2G7 M4XNRp4yOCEQvF2= NIS4eFBKdmirYnn0d{BE\WyuIG\pZYJqdGm2eR?= NXPIVGpbOjN2OEK2O|E>
Glioblastoma initiating cells NVnWZ|JJTnWwY4Tpc44h[XO|YYm= M1ywRZ4yOCEQvF2= NEW5UldqdmirYnn0d{Bv\XW{b4PwbIVz\SCob4LtZZRqd25? NV2zRoExOjN2OEK2O|E>
Glioblastoma initiating cells M2DONWN6fG:6aXPpeJkh[XO|YYm= M1nBV54yOCEQvF2= MlPabY5lfWOnczDhdI9xfG:|aYO= NUG2TJB5OjN2OEK2O|E>
Glioblastoma initiating cells NWjTXpp2TnWwY4Tpc44h[XO|YYm= M3vwOZ4yOCEQvF2= M17tRoRwf26{ZXf1cIF1\XNidHjlJHNJUCC|aXfuZYxqdmdicHH0bJdigQ>? NWXQ[5FJOjN2OEK2O|E>
Glioblastoma initiating cells MlPiSpVv[3Srb36gZZN{[Xl? M{\ke54yOCEQvF2= M3n3W2lvcGmkaYTzJJRp\SCHeIDy[ZN{cW:wIH;mJGdmdmW|IFnueo9tfmWmIHnuJG1icW62YXnubY5oKFCudYLpdI91\W6leR?= MWiyN|Q5OjZ5MR?=
Glioblastoma initiating cells NHTYOZZHfW6ldHnvckBie3OjeR?= NFjSUmR,OTBizszN MWLJcohq[mm2czDNc5RqdGm2eTygTY53[XOrb36sJIFv\CCPaXfyZZRqd25? NXfpU4Z3OjN2OEK2O|E>
LOX IMVI MXPGeY5kfGmxbjDhd5NigQ>? MWGxNEDPxE1? NWHp[ZdyTE2VTx?= M2HWTIlvcGmkaYTzJGhm\GenaH;nMWdNUSCyYYToe4F6 MWmyN|k{PTl{NR?=
UACC 257 MnjHSpVv[3Srb36gZZN{[Xl? NXrsb2t1OTBizszN MlXRSG1UVw>? M{XTfYlvcGmkaYTzJGhm\GenaH;nMWdNUSCyYYToe4F6 NWfEfnB{OjN7M{W5NlU>
LOX IMVI NUDjbFV2TnWwY4Tpc44h[XO|YYm= M{XTeFExKM7:TR?= NYCxXpBrTE2VTx?= M37FNolv\HWlZYOgS|Eh[2WubDDjfYNt\SCjcoLld5Q> MoXoNlM6OzV7MkW=
UACC 257 NUPxdnBUTnWwY4Tpc44h[XO|YYm= NXTVdFdxOTBizszN NVu5dFFyTE2VTx?= M3ry[Ylv\HWlZYOgS|Eh[2WubDDjfYNt\SCjcoLld5Q> MonwNlM6OzV7MkW=
LOX IMVI MnH1R5l1d3irY3n0fUBie3OjeR?= NGOwUYIyOCEQvF2= MnnISG1UVw>? M4D3R4Rm[3KnYYPld{B1fW2xcjDj[YxtKH[rYXLpcIl1gQ>? MmTWNlM6OzV7MkW=
UACC 257 NVfxZ2RkS3m2b4jpZ4l1gSCjc4PhfS=> M2XYTVExKM7:TR?= M2fHVWROW09? MmLQ[IVkemWjc3XzJJR2dW:{IHPlcIwhfmmjYnnsbZR6 M4XYUVI{QTN3OUK1
LOX IMVI NGnLOZpCeG:ydH;zbZMh[XO|YYm= NFHyOJYyOCEQvF2= MWDEUXNQ NGexNYZqdmS3Y3XzJIFxd3C2b4Ppdy=> MlnwNlM6OzV7MkW=
UACC 257 NEL3c4ZCeG:ydH;zbZMh[XO|YYm= NU\KRpFZOTBizszN MUPEUXNQ MW\pcoR2[2W|IHHwc5B1d3Orcx?= MlfCNlM6OzV7MkW=
ACHN MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{jNOp42KM7:TR?= NIi3c3NFVVOR NX7HS2I4UUN3ME2yMVPjiIoQvF2= NFzOXGYzPTB7M{S5NS=>
769-P MmnIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXPt[WpshjVizszN MVzEUXNQ NX;m[ZZpUUN3ME2yMVPjiIoQvF2= M3v6eVI2ODl|NEmx
786-O NV\UVYxUT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWnDOVAxhjVizszN M1H4R2ROW09? MnvpTWM2OD1{LURihKnPxE1? Mom0NlUxQTN2OUG=
786-O SuR NEG1SXFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnvUglUh|ryP NY\wbpJrTE2VTx?= M3PEb2lEPTB;Mj2z5qCK|ryP MUiyOVA6OzR7MR?=
SP53 M1OwU2Z2dmO2aX;uJIF{e2G7 NWToeIg{OzBizszN M1XNb2ROW09? MX7pcohq[mm2czDj[YxtKGGmaHXzbY9vKGGwZDDtbYdz[XSrb36= M1HCZlI3QDh3NkC4
SP53 MXfGeY5kfGmxbjDhd5NigQ>? MXuzNEDPxE1? NH3GTFFFVVOR MXLpcohq[mm2czD0bIUhXkyDND3t[YRq[XSnZDDGRWshe2mpbnHsbY5oKHCjdHj3ZZk> NXHnOXhxOjZ6OEW2NFg>
HS5 Mo[5SpVv[3Srb36gZZN{[Xl? NH\Q[VA{OCEQvF2= MULEUXNQ MXPpcohq[mm2czDj[YxtKGGmaHXzbY9vKGGwZDDtbYdz[XSrb36= NWLCN2dTOjZ6OEW2NFg>
HS27a MYHGeY5kfGmxbjDhd5NigQ>? NX7HdmxEOzBizszN M4TkV2ROW09? NFHLbopqdmirYnn0d{Bk\WyuIHHkbIV{cW:wIHHu[EBucWe{YYTpc44> NETYcpkzPjh6NU[wPC=>
SP53 NWrFR3M1S3m2b4jpZ4l1gSCjc4PhfS=> NW\qSmZTOzBizszN MWjEUXNQ MoHubY5lfWOnczDheZRweGijZ4m= MmWxNlY5QDV4MEi=
Jeko NVz3VFF[S3m2b4jpZ4l1gSCjc4PhfS=> MXyzNEDPxE1? M4n4NGROW09? MX;pcoR2[2W|IHH1eI9xcGGpeR?= 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]

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:
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
Synonyms

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01787552 Active, not recruiting Primary Myelofibrosis|Thrombocythemia, Essential|Thrombocytosis|Myeloproliferative Disorders|Bone Marrow Diseases|Hematologic Diseases|Blood Coagulation Disorders|Blood Platelet Disorders|Hemorrhagic Disorders Novartis Pharmaceuticals|Novartis May 8, 2013 Phase 1|Phase 2
NCT02254551 Terminated Multiple Myeloma SCRI Development Innovations, LLC|Novartis January 2015 Phase 2
NCT02138929 Recruiting Esophageal Cancer M.D. Anderson Cancer Center|Novartis|National Cancer Institute (NCI) November 2014 Phase 1
NCT02195973 Active, not recruiting Recurrent Ovarian Cancer University of Alabama at Birmingham|Novartis Pharmaceuticals September 2014 Phase 1
NCT02151864 Recruiting Hepatocellular Carcinoma|Cirrhosis Jason K. Sicklick, M.D.|Novartis Pharmaceuticals|University of California, San Diego July 2014 Phase 1
NCT02182622 Unknown status Prostate Cancer Martin Gutierrez|Novartis|Hackensack University Medical Center July 2014 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID