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.
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 MnnLR5l1d3irY3n0fUBie3OjeR?= M323Op4yOCEQvF2= MoK1TWM2OD1zMjFOwG0> NH;3e48zOjV3M{O1OS=>
A2780cp20 NYXXfWlkS3m2b4jpZ4l1gSCjc4PhfS=> MYP+NVAh|ryP NU\VfHlxUUN3ME23MlUh|ryP Mnf2NlI2PTN|NUW=
SKOV3ip1 NYC4VopvS3m2b4jpZ4l1gSCjc4PhfS=> Ml;PglExKM7:TR?= M4nYV2lEPTB;MkSg{txO NVnK[3Y6OjJ3NUOzOVU>
SKOV3TRip2 NFjtU5NEgXSxeHnjbZR6KGG|c3H5 MlrOglExKM7:TR?= Mlz1TWM2OD1zMjFOwG0> NUL2UmJIOjJ3NUOzOVU>
HeyA8 Mn7tR5l1d3irY3n0fUBie3OjeR?= MnfGglExKM7:TR?= M2HWN2lEPTB;MUig{txO MnezNlI2PTN|NUW=
HeyA8MDR NGHB[HVEgXSxeHnjbZR6KGG|c3H5 MVn+NVAh|ryP M3PCfGlEPTB;ODFOwG0> NFfhdoszOjV3M{O1OS=>
OS5 MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4TWc542KM7:TR?= NYHobpVvemWmdXPld{B1cGVicILvcIln\XKjdHnvci=> M3PINlI{OjR|NUm1
OS18 MnLMS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoT4glUh|ryP NEntcVlz\WS3Y3XzJJRp\SCycn;sbYZmemG2aX;u NEnpRZMzOzJ2M{W5OS=>
Glioblastoma initiating cells MVzDfZRwgGmlaYT5JIF{e2G7 MVT+NVAh|ryP MkPETY5pcWKrdIOgR4VtdCCYaXHibYxqfHl? MWSyN|Q5OjZ5MR?=
Glioblastoma initiating cells MXPGeY5kfGmxbjDhd5NigQ>? MUL+NVAh|ryP NWPLR3BZcW6qaXLpeJMhdmW3cn;zdIhmemViZn;ycYF1cW:w MnTuNlM1QDJ4N{G=
Glioblastoma initiating cells NHnvflJEgXSxeHnjbZR6KGG|c3H5 NG\oTnl,OTBizszN M2rWU4lv\HWlZYOgZZBweHSxc3nz NXP6SJRXOjN2OEK2O|E>
Glioblastoma initiating cells NILYZmFHfW6ldHnvckBie3OjeR?= MUn+NVAh|ryP Mnft[I94dnKnZ4XsZZRmeyC2aHWgV2hJKHOrZ37hcIlv\yCyYYToe4F6 NHz1V3AzOzR6Mk[3NS=>
Glioblastoma initiating cells NVSzT2hvTnWwY4Tpc44h[XO|YYm= MkTEglExKM7:TR?= NGTZVXJKdmirYnn0d{B1cGViRYjwdoV{e2mxbjDv[kBI\W6nczDJcpZwdH[nZDDpckBO[WmwdHHpcolv\yCSbIXybZBwfGWwY4m= MVWyN|Q5OjZ5MR?=
Glioblastoma initiating cells NF;WdJdHfW6ldHnvckBie3OjeR?= NFrEZZp,OTBizszN NGewcJJKdmirYnn0d{BOd3SrbHn0fUwhUW64YYPpc44tKGGwZDDNbYdz[XSrb36= NG\XfXEzOzR6Mk[3NS=>
LOX IMVI NHG3VWVHfW6ldHnvckBie3OjeR?= MXGxNEDPxE1? MmfRSG1UVw>? MnrjbY5pcWKrdIOgTIVl\2Wqb3etS2xKKHCjdHj3ZZk> MWmyN|k{PTl{NR?=
UACC 257 M1zBOWZ2dmO2aX;uJIF{e2G7 NFnTWYkyOCEQvF2= MWXEUXNQ M{jlOolvcGmkaYTzJGhm\GenaH;nMWdNUSCyYYToe4F6 NV\PO2pyOjN7M{W5NlU>
LOX IMVI M2TtRmZ2dmO2aX;uJIF{e2G7 MmLGNVAh|ryP NGryWnRFVVOR M3;uXYlv\HWlZYOgS|Eh[2WubDDjfYNt\SCjcoLld5Q> MX2yN|k{PTl{NR?=
UACC 257 MmDQSpVv[3Srb36gZZN{[Xl? M3TxUlExKM7:TR?= NVzaT2syTE2VTx?= M2jxbolv\HWlZYOgS|Eh[2WubDDjfYNt\SCjcoLld5Q> Mm\vNlM6OzV7MkW=
LOX IMVI M37hNWN6fG:6aXPpeJkh[XO|YYm= MkW5NVAh|ryP NFTacHhFVVOR NGm3b5hl\WO{ZXHz[ZMhfHWvb4KgZ4VtdCC4aXHibYxqfHl? Ml74NlM6OzV7MkW=
UACC 257 M{PFNmN6fG:6aXPpeJkh[XO|YYm= M1n3PVExKM7:TR?= NXiyZVhDTE2VTx?= MUDk[YNz\WG|ZYOgeJVud3JiY3XscEB3cWGkaXzpeJk> MVeyN|k{PTl{NR?=
LOX IMVI NX;VXJFZSXCxcITvd4l{KGG|c3H5 MYWxNEDPxE1? NXu5PVR[TE2VTx?= MljWbY5lfWOnczDhdI9xfG:|aYO= MmLwNlM6OzV7MkW=
UACC 257 NUfhfol{SXCxcITvd4l{KGG|c3H5 NXfE[|FXOTBizszN MYjEUXNQ MX7pcoR2[2W|IHHwc5B1d3Orcx?= NYnrR3dnOjN7M{W5NlU>
ACHN M2rLOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX;ISHlQhjVizszN MmX6SG1UVw>? Ml3MTWM2OD1{LURihKnPxE1? NU\YXZVmOjVyOUO0PVE>
769-P NVTpOVdPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmTwglUh|ryP NE\QbmRFVVOR NHO0RZRKSzVyPUKtN-KBkc7:TR?= MYWyOVA6OzR7MR?=
786-O NYDNSJBwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH\ORY5,PSEQvF2= NV;qVmtLTE2VTx?= M3;ve2lEPTB;Mj2z5qCK|ryP MmTJNlUxQTN2OUG=
786-O SuR MULHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVH+OUDPxE1? MVjEUXNQ NUO0T2Z7UUN3ME2yMVPjiIoQvF2= NH;tSGMzPTB7M{S5NS=>
SP53 MluySpVv[3Srb36gZZN{[Xl? NYO1TXc4OzBizszN NIXPZmNFVVOR MmLObY5pcWKrdIOgZ4VtdCCjZHjld4lwdiCjbnSgcYloemG2aX;u MXeyOlg5PTZyOB?=
SP53 MXzGeY5kfGmxbjDhd5NigQ>? MmHiN|Ah|ryP M1zFPWROW09? NILBbJhqdmirYnn0d{B1cGViVlzBOE1u\WSrYYTl[EBHSUtic3nncoFtcW6pIIDheIh4[Xl? NHu3[JgzPjh6NU[wPC=>
HS5 NGfndINHfW6ldHnvckBie3OjeR?= NUTBNnU3OzBizszN MorPSG1UVw>? NFLudG1qdmirYnn0d{Bk\WyuIHHkbIV{cW:wIHHu[EBucWe{YYTpc44> MWCyOlg5PTZyOB?=
HS27a MYTGeY5kfGmxbjDhd5NigQ>? MU[zNEDPxE1? MWLEUXNQ NGTyRW1qdmirYnn0d{Bk\WyuIHHkbIV{cW:wIHHu[EBucWe{YYTpc44> NVniZoRJOjZ6OEW2NFg>
SP53 MnHiR5l1d3irY3n0fUBie3OjeR?= M1fY[lMxKM7:TR?= NUP0V5FLTE2VTx?= MorpbY5lfWOnczDheZRweGijZ4m= NF6xXW4zPjh6NU[wPC=>
Jeko NH[1SJJEgXSxeHnjbZR6KGG|c3H5 MV[zNEDPxE1? MXjEUXNQ NHnvSJVqdmS3Y3XzJIF2fG:yaHHnfS=> NXX5ZYtTOjZ6OEW2NFg>

... 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
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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID