Art. -Nr.: HY-16582A

Sonidegib

(Synonyms: Erismodegib; LDE225; NVP-LDE225)

13 Cited Publications

Kundenbewertung

Based on 13 publication(s) in Google Scholar

Sonidegib (Erismodegib) is a potent and selective Smo antagonist with IC₅₀ of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively.

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Reinheit: 99.98%
CAS. Nr.: 956697-53-3
Formel: C₂₆H₂₆F₃N₃O₃
Molecular Weight:485.50

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Sonidegib Chemical Structure

CAS. Nr.: 956697-53-3

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Sonidegib (Erismodegib) is a potent and selective Smo antagonist with IC₅₀ of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively^[1].

IC₅₀ & Target

IC50: 1.3 nM (mSmo), 2.5 nM (hSmo)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	CC₅₀	2.26 μM Compound: LDE225	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay	10.21203/rs.3.rs-23951/v1
Caco-2	IC₅₀	10.67 μM Compound: LDE225	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging	10.21203/rs.3.rs-23951/v1
NIH3T3	IC₅₀	5.5 nM Compound: 2; LDE-225	Inhibition of Sonic-induced hedgehog signalling in mouse NIH3T3 cells after 48 hrs by Gli-luciferase reporter assay Inhibition of Sonic-induced hedgehog signalling in mouse NIH3T3 cells after 48 hrs by Gli-luciferase reporter assay	[PMID: 26820554]
NIH3T3	IC₅₀	5.5 nM Compound: LDE-225, NVP-LDE-225, sonidegib	Inhibition of SHH signaling pathway in mouse NIH3T3 cells measured after 48 hrs by Gli-luciferase reporter assay Inhibition of SHH signaling pathway in mouse NIH3T3 cells measured after 48 hrs by Gli-luciferase reporter assay	[PMID: 24176396]

In Vitro

The IC₅₀ values for Sonidegib (NVP-LDE225) for the major human CYP450 drug metabolizing enzymes is greater than 10 μM^[1]. Sonidegib (LDE225), a small molecule, clinically investigated SMO inhibitor, used alone and in combination with Nilotinib, inhibits the Hh pathway in CD34⁺ chronic phase (CP)-chronic myeloid leukaemia (CML) cells, reducing the number and self-renewal capacity of CML leukaemia stem cell (LSC). Sonidegib interacts directly with SMO, in a similar fashion to cyclopamine, to reduce expression of downstream Hh signaling targets. Primary CD34⁺ CP-CML cells are cultured in serum free media (SFM)±Sonidegib for 6, 24 and 72 hours (h). At 72 h, while there is variability between the biological samples, GLI1 is significantly downregulated following exposure to Sonidegib (10 nM; 0.78-fold and 100 nM; 0.73-fold, respectively (p<0.01)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Sonidegib (NVP-LDE225) is a weak base with a measured pK_a of 4.2 and exhibits relatively poor aqueous solubility. In the subcutaneous Ptch^+/-p53^-/- medulloblastoma allograft mouse model, Sonidegib demonstrates dose-related antitumor activity after 10 days of oral administration of a suspension of the diphosphate salt. At a dose of 5 mg/kg/day qd, Sonidegib significantly inhibits tumor growth, corresponding to a T/C value of 33% (p<0.05 as compared to vehicle controls). When dosed at 10 and 20 mg/kg/day qd, Sonidegib affords 51 and 83% regression, respectively^[1]. Bone marrow cells and spleen cells from a subset of treated mice are transplanted into secondary recipient mice. Transplantation of either bone marrow (BM) or spleen cells from mice treated with Sonidegib (LDE225)+Nilotinib results in reduced white cell count (WCC) and reduces leukaemia development in secondary recipients compared to Sonidegib or Nilotinib alone^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 956697-53-3
Appearance Solid
Molecular Weight 485.50
Formel C₂₆H₂₆F₃N₃O₃
Color White to light yellow
SMILES

O=C(C1=C(C)C(C(C=C2)=CC=C2OC(F)(F)F)=CC=C1)NC3=CC=C(N=C3)N4C[C@@H](C)O[C@@H](C)C4
Synonyms

Erismodegib; LDE225; NVP-LDE225
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (13)

All In Vivo Efficacy StudyWBHistological Imaging/StainingIF

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Journal Impact Factor

Nat Med

A biobank of patient-derived pediatric brain tumor models. [Abstract]

2018 Nov;24(11):1752-1761. PMID: 30349086
Free Radic Biol Med

Targeted delivery of nebivolol via lactoferrin-modified liposomes inhibits NEK7-mediated pyroptosis to ameliorate inflammatory bowel disease. [Abstract]

2026 Aug 16:252:493-508. PMID: 42061481
J Genet Genomics

Reduced Smoothened level rescues Aβ-induced memory deficits and neuronal inflammation in animal models of Alzheimer's disease. [Abstract]

2018 May 20;45(5):237-246. PMID: 29807798

Sonidegib purchased from MedChemExpress. Usage Cited in: J Genet Genomics. 2018 May 20;45(5):237-246. [Abstract]

Drug-feeding scheme (upper panel). Memory rescuing effects through treatment with LDE225 (LDE) or Vismodegib (VIS) at 20 mg/kg for 7.5-m-old and 15-m-old mice (lower panel, n=7 for each group).
J Pathol

Transcriptomic profiling reveals the role of Hedgehog signaling as a biomarker and in the pathogenesis of Ménétrier's disease. [Abstract]

2025 Nov 6. PMID: 41199529

Sonidegib purchased from MedChemExpress. Usage Cited in: J Pathol. 2025 Nov 6. [Abstract]

Sonidegib (5 mg/kg; IP; three weeks every other day) in Two-to-four-month-old MT-TGFα mice showed Sonidegib or DMSO treatment did not affect the weight of mice.

Sonidegib purchased from MedChemExpress. Usage Cited in: J Pathol. 2025 Nov 6. [Abstract]

Sonidegib (5 mg/kg; IP; three weeks every other day) in Two-to-four-month-old MT-TGFα mice showed immunoblotting with anti-GLI1 and anti-beta-actin antibodies showed GLI1 expression is decreased by the sonidegib treatment, confirming the effective inhibition of Hh signaling. Bar graph represents quantification of the immunoblotting.

Sonidegib purchased from MedChemExpress. Usage Cited in: J Pathol. 2025 Nov 6. [Abstract]

Sonidegib (5 mg/kg; IP; three weeks every other day) in Two-to-four-month-old MT-TGFα mice showed Hematoxylin and eosin (H&E) stains reveal that Hh inhibitor sonidegib treatment partially rescues the phenotypes in MT-TGFα mice.

Sonidegib purchased from MedChemExpress. Usage Cited in: J Pathol. 2025 Nov 6. [Abstract]

Sonidegib (5 mg/kg; IP; three weeks every other day) in Two-to-four-month-old MT-TGFα mice showed H+/K+ ATPase positive parietal cells and GIF positive chief cells are significantly increased following sonidegib treatment. UEA1 positive foveolar cells are significantly decreased while GSII positive neck cells show a decreasing trend although the result is not statistically significant. The Ki-67 positive proliferating cells are significantly decreased after sonidegib treatment in stomach tissues.

Sonidegib purchased from MedChemExpress. Usage Cited in: J Pathol. 2025 Nov 6. [Abstract]

Immunofluorescentstaining shows GLI1 expression is decreased following Sonidegib (50 μM; 48 h) treatment whereas pEGFR expression is not changing in gastric organoids from MD patients.

Sonidegib purchased from MedChemExpress. Usage Cited in: J Pathol. 2025 Nov 6. [Abstract]

Immunoblotting with anti-pEGFR, anti-GLI1, and anti-b-actin antibodies show GLI1 expression is significantly decreased in the Sonidegib (50 μM; 48 h) treatment group whereas pEGFR expression is not changing in gastric organoids from MD patients. Bar graphs represent quantification of the immunoblotting.
Tissue Cell

U0126 induces osteoclast differentiation via the p38-NFATc-1 signaling pathway. [Abstract]

2026 Apr:99:103263. PMID: 41365188
Tissue Cell

The Shh-p38-NFATc1 signaling pathway is essential for osteoclastogenesis during tooth eruption. [Abstract]

2025 Feb:92:102643. PMID: 39612595
Cell Physiol Biochem

Sonidegib, a Novel Inhibitor of Suicidal Erythrocyte Death. [Abstract]

2018;47(4):1352-1364. PMID: 29929201
bioRxiv

2025 Oct 11.
SSRN

2025 Jul 25.
bioRxiv

2024 Jul 25.
bioRxiv

The molecular chronology of mammary epithelial cell fate switching. [Abstract]

2024 Nov 4:2024.10.08.617155. PMID: 39415993
bioRxiv

Transcriptomic Profiling Reveals Claudin 18.2 as a Diagnostic Biomarker of Ménétrier's Disease and the Role of Hedgehog Signaling in Pathogenesis. [Abstract]

2023 Nov 6:2023.11.03.565570. PMID: 37986961
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (205.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0597 mL

10.2987 mL

20.5973 mL

5 mM

0.4119 mL

2.0597 mL

4.1195 mL

10 mM

0.2060 mL

1.0299 mL

2.0597 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.15 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 75% PEG300 25% (5% Dextrose in Water)

Solubility: 2 mg/mL (4.12 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[2]

CD34⁺ CP-CML cells are seeded in SFM alone±Sonidegib±Nilotinib and cultured for 24-72 h prior to assessment. Proliferation is measured using colorimetric assessment of BrDU incorporation. Proportion of viable cells versus those in early and late apoptosis is assessed by flow cytometry using annexin V-FITC and 7-amino-actinomycin D (7-AAD, Via-Probe solution). Cell cycle status is assessed using Ki67 (FITC) expression and 7-AAD incorporation.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

Mice^[2]
The transgenic EGFP⁺/SCLtTA/TRE-BCR-ABL mouse model is used to investigate the effect of Sonidegib treatment on CML LSC in vivo. Scl-tTa-BCR-ABL mice in the FVB/N background are crossed with transgenic GFP-expressing mice. Bone marrow cells are obtained 4 weeks post induction, GFP⁺ cells are selected by flow cytometry and transplanted by tail vein injection (10⁶ cells/mouse) into wild-type FVB/N recipient mice, irradiated at 900 cGy, generating a large cohort of mice with similar time of onset of leukemia. Blood samples obtained 4 weeks post transplantation confirmed a neutrophilic leukocytosis in recipient mice. Mice are treated with Nilotinib (50 mg/kg by gavage, daily), Sonidegib (80 mg/kg by gavage, daily), Sonidegib+Nilotinib, or with vehicle alone (control). After 3 weeks of treatment, animals are euthanised and marrow content of femurs and tibiae, spleen cells and blood obtained. Total white cell count (WCC), GFP-expressing WCC, myeloid cells, and GFP+ progenitors and stem cells are measured by flow cytometry. Survival is assessed in a subset of mice for 120d post discontinuation of treatment. Spleen and BM cells from a subset of mice in each arm are pooled and 5×10⁶ cells/mouse (8 mice/condition) are transplanted into wild-type FVB/N recipient mice irradiated at 900 cGy. Engraftment is monitored by drawing peripheral blood (PB) every 4 weeks. The percentage of GFP⁺ cells in PB is analyzed by flow cytometry.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Pan S, et al. Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist. ACS Med Chem Lett. 2010 Mar 16;1(3):130-4. [Content Brief]

[2]. Irvine DA, et al. Deregulated hedgehog pathway signaling is inhibited by the smoothened antagonist LDE225 (Sonidegib) in chronic phase chronic myeloid leukaemia. Sci Rep. 2016 May 9;6:25476. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0597 mL	10.2987 mL	20.5973 mL	51.4933 mL
	5 mM	0.4119 mL	2.0597 mL	4.1195 mL	10.2987 mL
	10 mM	0.2060 mL	1.0299 mL	2.0597 mL	5.1493 mL
	15 mM	0.1373 mL	0.6866 mL	1.3732 mL	3.4329 mL
	20 mM	0.1030 mL	0.5149 mL	1.0299 mL	2.5747 mL
	25 mM	0.0824 mL	0.4119 mL	0.8239 mL	2.0597 mL
	30 mM	0.0687 mL	0.3433 mL	0.6866 mL	1.7164 mL
	40 mM	0.0515 mL	0.2575 mL	0.5149 mL	1.2873 mL
	50 mM	0.0412 mL	0.2060 mL	0.4119 mL	1.0299 mL
	60 mM	0.0343 mL	0.1716 mL	0.3433 mL	0.8582 mL
	80 mM	0.0257 mL	0.1287 mL	0.2575 mL	0.6437 mL
	100 mM	0.0206 mL	0.1030 mL	0.2060 mL	0.5149 mL

Keywords

Sonidegib

13 Cited Publications

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Sonidegib

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Pancreatic Cancer Compound Library

Targeted Therapy Drug Library

Anti-Liver Cancer Compound Library

Rare Diseases Drug Library

Anti-Colorectal Cancer Compound Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Sonidegib

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Sonidegib

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Pancreatic Cancer Compound Library

Targeted Therapy Drug Library

Anti-Liver Cancer Compound Library

Rare Diseases Drug Library

Anti-Colorectal Cancer Compound Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Sonidegib

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Sonidegib Related Classifications

HY-16582A Related Classifications