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[CAS NO. 1218778-77-8] Sonidegibdiphosphate

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

Overview

MDL	-
Molecular Weight	681.49
Molecular Formula	C26H32F3N3O11P2
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.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

[1]Nat Med. 2018 Nov;24(11):1752-1761.
[2]J Genet Genomics. 2018 May 20;45(5):237-246.
[3]Patent. US20180263995A1.
[4]Cell Physiol Biochem. 2018;47(4):1352-1364.

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
NCT01787552	Novartis Pharmaceuticals\|Novartis	Primary Myelofibrosis\|Thrombocytosis\|Essential Thrombocythemia\|Polycythemia Vera\|Myeloproliferative Disorders\|Bone Marrow Diseases\|Hematologic Diseases\|Blood Coagulation Disorders\|Blood Platelet Disorders\|Hemorrhagic Disorders	May 8, 2013	Phase 1\|Phase 2
NCT01708174	Novartis Pharmaceuticals\|Novartis	Medulloblastoma	May 6, 2013	Phase 2
NCT02182622	Martin Gutierrez\|Novartis\|Hackensack Meridian Health	Prostate Cancer	July 2014	Phase 1
NCT00961896	Novartis Pharmaceuticals\|Novartis	Treatment for Basal Cell Carcinomas (BCCs) in Gorlin Syndrome Patients	July 2009	Phase 2
NCT01911416	University of Utah	Pancreatic Ductal Adenocarcinoma	January 2014	Not Applicable
NCT02027376	Spanish Breast Cancer Research Group\|Novartis	Advanced Breast Cancer	May 2014	Phase 1
NCT02086552	Mayo Clinic\|National Cancer Institute (NCI)\|Novartis Pharmaceuticals	Recurrent Plasma Cell Myeloma\|Refractory Plasma Cell Myeloma	January 17, 2014	Phase 2
NCT03534947	Melanoma Institute Australia	Basal Cell Carcinoma\|Basal Cell Carcinoma of Skin, Site Unspecified\|Skin Cancer\|Invasive Carcinoma	July 23, 2019	Phase 2
NCT01350115	Novartis Pharmaceuticals\|Novartis	Basal Cell Carcinoma\|Gorlin Syndrome\|Nevoid Basal Cell Carcinoma Syndrome	April 2011	Phase 2
NCT02086513	Massachusetts General Hospital\|Novartis	Graft Versus Host Disease	April 2014	Phase 1
NCT02002689	Novartis Pharmaceuticals\|Novartis	PTCH1 or SMO Activated Solid and Hematologic Tumors	February 2014	Phase 2
NCT04007744	Mayo Clinic\|National Cancer Institute (NCI)	Clinical Stage III Cutaneous Melanoma AJCC v8\|Clinical Stage III Gastric Cancer AJCC v8\|Clinical Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8\|Clinical Stage IV Cutaneous Melanoma AJCC v8\|Clinical Stage IV Gastric Cancer AJCC v8\|Clinical Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8\|Clinical Stage IVA Gastric Cancer AJCC v8\|Clinical Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Clinical Stage IVB Gastric Cancer AJCC v8\|Clinical Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Locally Advanced Urothelial Carcinoma\|Metastatic Gastric Adenocarcinoma\|Metastatic Gastroesophageal Junction Adenocarcinoma\|Metastatic Head and Neck Squamous Cell Carcinoma\|Metastatic Lung Non-Small Cell Carcinoma\|Metastatic Malignant Solid Neoplasm\|Metastatic Melanoma\|Metastatic Urothelial Carcinoma\|Pathologic Stage III Cutaneous Melanoma AJCC v8\|Pathologic Stage III Gastric Cancer AJCC v8\|Pathologic Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IIIA Gastric Cancer AJCC v8\|Pathologic Stage IIIA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IIIB Gastric Cancer AJCC v8\|Pathologic Stage IIIB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IIIC Gastric Cancer AJCC v8\|Pathologic Stage IV Cutaneous Melanoma AJCC v8\|Pathologic Stage IV Gastric Cancer AJCC v8\|Pathologic Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Recurrent Head and Neck Squamous Cell Carcinoma\|Refractory Lung Non-Small Cell Carcinoma\|Stage IV Cutaneous Squamous Cell Carcinoma of the Head and Neck AJCC v8\|Stage IV Lung Cancer AJCC v8\|Stage IVA Lung Cancer AJCC v8\|Stage IVB Lung Cancer AJCC v8\|Unresectable Malignant Solid Neoplasm\|Unresectable Melanoma	February 13, 2020	Phase 1
NCT04402073	European Organisation for Research and Treatment of Cancer - EORTC	Medulloblastoma	November 11, 2022	Phase 2
NCT02254551	SCRI Development Innovations, LLC\|Novartis	Multiple Myeloma	January 2015	Phase 2
NCT01033019	Novartis Pharmaceuticals\|Novartis	Sporadic Superficial and Nodular Skin Basal Cell Carcinomas	December 2009	Phase 2
NCT02303041	Anne Chang\|Novartis Pharmaceuticals\|Stanford University	Carcinoma, Basal Cell\|Recurrent Skin Cancer\|Skin Neoplasms\|Basal Cell Nevus Syndrome	February 2015	Phase 2
NCT01208831	Novartis Pharmaceuticals\|Novartis	Advanced Solid Tumor Cancers\|Medulloblastoma\|Basal Cell Carcinoma	October 2010	Phase 1
NCT01769768	Novartis Pharmaceuticals\|Novartis	Advanced Solid Tumor	April 2013	Phase 1
NCT02195973	University of Alabama at Birmingham\|Novartis Pharmaceuticals	Recurrent Ovarian Cancer	September 2014	Phase 1
NCT02129101	Mayo Clinic\|National Cancer Institute (NCI)	Chronic Myelomonocytic Leukemia\|de Novo Myelodysplastic Syndrome\|Essential Thrombocythemia\|Myelodysplastic Syndrome\|Myelodysplastic+Myeloproliferative Neoplasm\|Polycythemia Vera\|Previously Treated Myelodysplastic Syndrome\|Primary Myelofibrosis\|Recurrent Adult Acute Myeloid Leukemia\|Recurrent Childhood Acute Myeloid Leukemia\|Untreated Adult Acute Myeloid Leukemia	May 2014	Phase 1
NCT01327053	Novartis Pharmaceuticals\|Novartis	Basal Cell Carcinoma	June 29, 2011	Phase 2
NCT02111187	Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins	Prostate Cancer	April 2014	Phase 1
NCT01529450	Anne Chang\|Novartis\|Stanford University	Basal Cell Carcinoma	February 2012	Not Applicable
NCT01826214	Novartis Pharmaceuticals\|Novartis	Acute Leukemias	May 2013	Phase 2
NCT03434262	St. Jude Children´s Research Hospital\|Novartis Pharmaceuticals	Anaplastic Astrocytoma\|Anaplastic Ependymoma\|Anaplastic Ganglioglioma\|Anaplastic Meningioma\|Anaplastic Oligodendroglioma\|Pleomorphic Xanthoastrocytoma, Anaplastic\|Atypical Teratoid+Rhabdoid Tumor\|Brain Cancer\|Brain Tumor\|Central Nervous System Neoplasms\|Choroid Plexus Carcinoma\|CNS Embryonal Tumor With Rhabdoid Features\|Ganglioneuroblastoma of Central Nervous System\|CNS Tumor\|Embryonal Tumor of CNS\|Ependymoma\|Glioblastoma\|Glioma\|Glioma, Malignant\|Medulloblastoma\|Medulloblastoma; Unspecified Site\|Medulloepithelioma\|Neuroepithelial Tumor\|Neoplasms\|Neoplasms, Neuroepithelial\|Papillary Tumor of the Pineal Region (High-grade Only)\|Pediatric Brain Tumor\|Pineal Parenchymal Tumor of Intermediate Differentiation (High-grade Only)\|Pineoblastoma\|Primitive Neuroectodermal Tumor\|Recurrent Medulloblastoma\|Refractory Brain Tumor\|Neuroblastoma. CNS\|Glioblastoma, IDH-mutant\|Glioblastoma, IDH-wildtype\|Medulloblastoma, Group 3\|Medulloblastoma, Group 4\|Glioma, High Grade\|Neuroepithelial Tumor, High Grade\|Medulloblastoma, SHH-activated and TP53 Mutant\|Medulloblastoma, SHH-activated and TP53 Wildtype\|Medulloblastoma, Chromosome 9q Loss\|Medulloblastoma, Non-WNT Non-SHH, NOS\|Medulloblastoma, Non-WNT+Non-SHH\|Medulloblastoma, PTCH1 Mutation\|Medulloblastoma, WNT-activated\|Ependymoma, Recurrent\|Glioma, Recurrent High Grade\|Glioma, Recurrent Malignant\|Embryonal Tumor, NOS\|Glioma, Diffuse Midline, H3K27M-mutant\|Embryonal Tumor With Multilayered Rosettes (ETMR)\|Ependymoma, NOS, WHO Grade III\|Ependymoma, NOS, WHO Grade II\|Medulloblastoma, G3+G4\|Ependymoma, RELA Fusion Positive	March 5, 2018	Phase 1
NCT00880308	Novartis Pharmaceuticals\|Novartis	Advanced Solid Tumor Cancers\|Medulloblastoma\|Basal Cell Carcinoma	March 2009	Phase 1
NCT01125800	Novartis Pharmaceuticals\|Novartis	Medulloblastoma\|Rhabdomyosarcoma\|Neuroblastoma\|Hepatoblastoma\|Glioma\|Astrocytoma	February 2011	Phase 1\|Phase 2
NCT01694589	Rutgers, The State University of New Jersey\|Rutgers Cancer Institute of New Jersey\|National Cancer Institute (NCI)\|Novartis Pharmaceuticals	Resectable Pancreatic Cancer	November 2012	Early Phase 1
NCT05463757	Maastricht University Medical Center\|Sun Pharmaceutical Industries Limited	Basal Cell Carcinoma\|Locally Advanced Basal Cell Carcinoma\|Metastatic Basal Cell Carcinoma\|Gorlin Syndrome\|Basal Cell Nevus Syndrome\|Carcinoma, Basal Cell\|Carcinoma\|Basal Cell Tumor\|Skin Cancer\|Neoplasm of Skin\|Neoplasms, Basal Cell	November 1, 2021
NCT01954355	Swiss Group for Clinical Cancer Research	Solid Tumor\|Ovarian Cancer	September 2013	Phase 1
NCT01757327	Washington University School of Medicine	Breast Neoplasms	April 2014	Phase 2
NCT04066504	Sun Pharmaceutical Industries Limited	Basal Cell Carcinoma	March 11, 2019
NCT01576666	Novartis Pharmaceuticals\|Novartis	Dose Escalation\|Safety\|Preliminary Efficacy\|Advanced Solid Tumors\|Metastatic Breast Cancer\|Advanced Pancreatic Adenocarcinoma\|Metastatic Colorectal Cancer\|Recurrent Glioblastoma Multiforme\|Gastric Cancer\|Gastroesophageal Junction Cancer\|Triple Negative Metastatic Breast Cancer\|Hormone Receptor Positive (ER&addition;+PR&addition;, and Her2-) Metastatic Breast Cancer	July 2012	Phase 1
NCT04806646	Gruppo Oncologico del Nord-Ovest	Locally Advanced Basal Cell Carcinoma	January 12, 2021	Phase 2
NCT02151864	Jason K. Sicklick, M.D.\|Novartis Pharmaceuticals\|University of California, San Diego	Hepatocellular Carcinoma\|Cirrhosis	July 2014	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.

References

[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.
[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.

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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