Sonidegib (NVP-LDE225)
For research use only. Not for use in humans.
Catalog No.S2151 Synonyms: Erismodegib
27 publications
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.
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. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Targets |
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| 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] |
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| Cell Data |
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| Assay |
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| 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: |
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| Animal Research: |
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Solubility (25°C)
| In vitro | DMSO | 97 mg/mL (199.79 mM) |
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| 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 | Erismodegib |
| Smiles | CC1CN(CC(C)O1)C2=CC=C(NC(=O)C3=C(C)C(=CC=C3)C4=CC=C(OC(F)(F)F)C=C4)C=N2 |
Bio Calculators
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Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT02254551 | Terminated | Drug: LDE225|Drug: Bortezomib | Multiple Myeloma | SCRI Development Innovations LLC|Novartis | January 2015 | Phase 2 |
| NCT02138929 | Active not recruiting | Drug: Everolimus|Drug: LDE 225 | Esophageal Cancer | M.D. Anderson Cancer Center|Novartis|National Cancer Institute (NCI) | November 10 2014 | Phase 1 |
| NCT02195973 | Completed | Drug: LDE225 | Recurrent Ovarian Cancer | University of Alabama at Birmingham|Novartis Pharmaceuticals | September 2014 | Phase 1 |
| NCT02027376 | Completed | Drug: LDE225|Drug: Docetaxel | Advanced Breast Cancer | Spanish Breast Cancer Research Group|Novartis | May 2014 | Phase 1 |
| NCT02111187 | Completed | Drug: LDE225 | Prostate Cancer | Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins | April 2014 | Phase 1 |
| NCT02086513 | Terminated | Drug: LDE225 | Graft Versus Host Disease | Massachusetts General Hospital|Novartis | April 2014 | Phase 1 |
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