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[CAS NO. 956697-53-3]  Sonidegib

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PRODUCTS SPECIFICATIONS [956697-53-3]

Catalog
HY-16582A
Brand
MCE
CAS
956697-53-3

DESCRIPTION [956697-53-3]

Overview

MDLMFCD16038928
Molecular Weight485.50
Molecular FormulaC26H26F3N3O3
SMILESO=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

For research use only. We do not sell to patients.

4 Publications Citing Use of MCE


Summary

Sonidegib (Erismodegib) is a potent and selective Smo antagonist with IC 50 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]


In Vitro

The IC 50 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] .

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] .

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


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT01125800 Novartis Pharmaceuticals|Novartis
Medulloblastoma|Rhabdomyosarcoma|Neuroblastoma|Hepatoblastoma|Glioma|Astrocytoma
February 2011 Phase 1|Phase 2
NCT01911416 University of Utah
Pancreatic Ductal Adenocarcinoma
January 2014 Not Applicable
NCT01764776 Novartis Pharmaceuticals|Novartis
Normal Hepatic Function|Impaired Hepatic Function
March 2013 Phase 1

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 102.99 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

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

* All of the co-solvents are available by MCE.


Synonyms

[1,1′-Biphenyl]-3-carboxamide, N-[6-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-3-pyridinyl]-2-methyl-4′-(trifluoromethoxy)-, rel-
rel-N-[6-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-3-pyridinyl]-2-methyl-4′-(trifluoromethoxy)[1,1′-biphenyl]-3-carboxamide
NVP-LDE 225
LDE 225
Sonidegib

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