LDE225 (NVP-LDE225,Erismodegib)

Catalog No.S2151

LDE225 (NVP-LDE225,Erismodegib) 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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LDE225 (NVP-LDE225,Erismodegib) Chemical Structure

LDE225 (NVP-LDE225,Erismodegib) Chemical Structure
Molecular Weight: 485.5

Validation & Quality Control

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Related Compound Libraries

LDE225 (NVP-LDE225,Erismodegib) is available in the following compound libraries:

Hedgehog/Smoothened Inhibitors with Unique Features

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  • Smoothened Inhibitor in Clinical Trial

    LDE225 (NVP-LDE225,Erismodegib) Phase III for Hh-pathway activated relapsed Medulloblastoma (MB).

  • Newest Smoothened Inhibitor

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Product Information

  • Compare Hedgehog/Smoothened Inhibitors
    Compare Hedgehog/Smoothened Products
  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description LDE225 (NVP-LDE225,Erismodegib) 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)
IC50 1.3 nM 2.5 nM
In vitro 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
Glioblastoma initiating cellsM4[5OmN6fG:6aXPpeJkh[XO|YYm=MVf+NVAh|ryPMUPJcohq[mm2czDD[YxtKF[rYXLpcIl1gQ>?NFTlTXUzOzR6Mk[3NS=>
Glioblastoma initiating cellsMoHBSpVv[3Srb36gZZN{[Xl?MXr+NVAh|ryPMkPybY5pcWKrdIOgcoV2em:|cHjldoUh\m:{bXH0bY9vNH;VdpUzOzR6Mk[3NS=>
Glioblastoma initiating cellsMnfoR5l1d3irY3n0fUBie3OjeR?=NHzCNnV,OTBizszNNFjTPWpqdmS3Y3XzJIFxd3C2b4Ppdy=>M{PtRlI{PDh{Nkex
Glioblastoma initiating cellsNYC3dXBETnWwY4Tpc44h[XO|YYm=Ml;FglExKM7:TR?=NGPFOW1ld3ewcnXneYxifGW|IITo[UBUUEhic3nncoFtcW6pIIDheIh4[Xl?M1L0NFI{PDh{Nkex
Glioblastoma initiating cellsMXXGeY5kfGmxbjDhd5NigQ>?NFjTOJl,OTBizszNNILnfIlKdmirYnn0d{B1cGViRYjwdoV{e2mxbjDv[kBI\W6nczDJcpZwdH[nZDDpckBO[WmwdHHpcolv\yCSbIXybZBwfGWwY4m=NWT6S2tYOjN2OEK2O|E>
Glioblastoma initiating cellsNH3BcFNHfW6ldHnvckBie3OjeR?=NIL4TmF,OTBizszNMXPJcohq[mm2czDNc5RqdGm2eTygTY53[XOrb36sJIFv\CCPaXfyZZRqd25?MoDKNlM1QDJ4N{G=
UACC 257M2nrOWZ2dmO2aX;uJIF{e2G7NWXBfohEOTBizszNM2f3NmROW09?MoXibY5pcWKrdIOgTIVl\2Wqb3etS2xKKHCjdHj3ZZk>NXH1[GxwOjN7M{W5NlU>
UACC 257NUDte2FKTnWwY4Tpc44h[XO|YYm=NHjyeYgyOCEQvF2=NX35TnROTE2VTx?=NYexeVNGcW6mdXPld{BIOSClZXzsJIN6[2ynIHHydoV{fA>?MmnsNlM6OzV7MkW=
UACC 257NIPuO4ZEgXSxeHnjbZR6KGG|c3H5MXSxNEDPxE1?NWrSOWZ1TE2VTx?=MlWz[IVkemWjc3XzJJR2dW:{IHPlcIwhfmmjYnnsbZR6MYSyN|k{PTl{NR?=
UACC 257M1PRdGFxd3C2b4Ppd{Bie3OjeR?=NYPDflB7OTBizszNMlmxSG1UVw>?M4nsd4lv\HWlZYOgZZBweHSxc3nzNUnTV4JqOjN7M{W5NlU>

... Click to View More Cell Line Experimental Data

In vivo 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(Only for Reference)

Cell Assay: [1]

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

Animal Study: [1]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Pan SF, et al. ACS Med. Chem. Lett., 2010, 1 (3), 130–134.

[2] Fendrich V, et al. Ann Surg, 2011, 254(5), 818-23.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
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 Inst  ...more M.D. Anderson Cancer Center|Novartis|National Cancer Institute (NCI) November 2014 Phase 1
NCT02195973 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|Universi  ...more Jason K. Sicklick, M.D.|Novartis Pharmaceuticals|University of California, San Diego July 2014 Phase 1
NCT02182622 Not yet recruiting Prostate Cancer Martin Gutierrez|Novartis|Hackensack University Medical C  ...more Martin Gutierrez|Novartis|Hackensack University Medical Center July 2014 Phase 1

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Chemical Information

Download LDE225 (NVP-LDE225,Erismodegib) SDF
Molecular Weight (MW) 485.5


CAS No. 956697-53-3
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms Sonidegib
Solubility (25°C) * In vitro DMSO 97 mg/mL (199.79 mM)
Ethanol 97 mg/mL warming (199.79 mM)
Water <1 mg/mL (<1 mM)
In vivo 2% DMSO+corn oil 10mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name [1,1'-Biphenyl]-3-carboxamide, N-[6-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-3-pyridinyl]-2-methyl-4'-(trifluoromethoxy)-, rel-

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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