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Sonidegib

Catalog No. T1926 CAS 956697-53-3

Synonyms: Erismodegib, NVP-LDE225, LDE225

Sonidegib (Erismodegib), a Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively.

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Sonidegib, CAS 956697-53-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 54.00
10 mg	In stock	$ 76.00
25 mg	In stock	$ 118.00
50 mg	In stock	$ 164.00
100 mg	In stock	$ 274.00
1 mL * 10 mM (in DMSO)	In stock	$ 58.00

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Purity: 99.97%

Purity: 99.91%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Sonidegib (Erismodegib), a Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively.
Targets&IC50	Smo (mouse):1.3 nM, Smo (human):2.5 nM
In vitro	The PAMPA experiment revealed that LDE225 possesses a permeability of up to 90.8%. In gradient dilution tests across clinical species, LDE225 demonstrated high oral bioavailability, with biological efficacy ranging from 69% to 102%. LDE225 is weakly basic (pKa: 4.20) and exhibits relatively poor water solubility. The compound shows dose-dependent antitumor activity. It strongly binds to plasma proteins in rats, mice, and humans (>99%), and exhibits binding capacities of 77% and 85% with dog and monkey plasma proteins, respectively. In the Rip1-Tag2 mouse model, LDE225 significantly reduced tumor volume by 95.7%. Administered at a dosage of 5 mg/kg/day, it significantly inhibited tumor growth, equivalent to a 33% T/C value. At dosages of 10 or 20 mg/kg/day, LDE225 achieved tumor regression effects of 51% and 83%, respectively. The inhibition of Gli1 mRNA is associated with the contact between the tumor and plasma mediated by LDE225. In an animal model with tumor transplantation, LDE225 was able to cross the blood-brain barrier and inhibit tumor growth after four days of treatment.
In vivo	LDE 225 (0.6-0.8 μM) inhibits the TM3 fluorescent reporter cell line, which has been treated with Hh agonists Ag1.5 ranging from 1 nM to 25 nM.
Cell Research	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)

Synonyms	Erismodegib, NVP-LDE225, LDE225
Molecular Weight	485.5
Formula	C26H26F3N3O3
CAS No.	956697-53-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90 mg/mL (185.4 mM)

Ethanol: 90 mg/mL (185.4 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

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. 3. Tauchi T, et al. Arthritis Res Ther, 2012, 14(Suppl 1), O43.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library EMA Approved Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library GPCR Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max

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Keywords

Sonidegib 956697-53-3 GPCR/G Protein Stem Cells Hedgehog/Smoothened Smo NVP-LDE-225 LDE-225 Erismodegib Inhibitor inhibit Smoothened LDE 225 NVP-LDE225 NVP-LDE 225 LDE225 inhibitor

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