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[CAS NO. 1218778-77-8]  Sonidegibdiphosphate

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PRODUCTS SPECIFICATIONS [1218778-77-8]

Catalog
HY-16582
Brand
MCE
CAS
1218778-77-8

DESCRIPTION [1218778-77-8]

Overview

MDL-
Molecular Weight681.49
Molecular FormulaC26H32F3N3O11P2
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.O=P(O)(O)O.O=P(O)(O)O

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

4 Publications Citing Use of MCE


Summary

Sonidegib diphosphate (Erismodegib diphosphate) 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
NCT01764776 Novartis Pharmaceuticals|Novartis
Normal Hepatic Function|Impaired Hepatic Function
March 2013 Phase 1
NCT02138929 M.D. Anderson Cancer Center|Novartis|National Cancer Institute (NCI)
Esophageal Cancer
November 10, 2014 Phase 1
NCT01456676 Novartis Pharmaceuticals|Novartis
Philadelphia Chromosome Positive Chronic Myelogenous Leukemia
January 2012 Phase 1

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)


Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 146.74 mM ; Need ultrasonic)

H 2 O : 0.25 mg/mL ( 0.37 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4674 mL 7.3369 mL 14.6737 mL
5 mM 0.2935 mL 1.4674 mL 2.9347 mL
10 mM 0.1467 mL 0.7337 mL 1.4674 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 (3.67 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (3.67 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (3.67 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-, phosphate (1:2)
Sonidegib phosphate
LDE 225 phosphate
Odomzo

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