LDE225 (phosphate)

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LDE225 (phosphate)

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Cat No: 16263

Biochemicals - Receptor Pharmacology

Hedgehog (Hh) proteins, important regulators of development, bind the cell-surface protein Patched, allowing activation of the GPCR-like receptor, Smoothened (SMO).{21774} In vertebrates, this ultimately leads to the activation of the zinc-finger trans...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

rel-N-[6-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-3-pyridinyl]-2-methyl-4'-(trifluoromethoxy)-[1,1'-biphenyl]-3-carboxamide, diphosphate

Correlated keywords:

956697-53-3 1218778-76-7 1218778-78-9 1270169-93-1 7664-38-2 28602-75-7 178560-73-1 959699-83-3 1021417-41-3 1053657-23-0 1196963-54-8 cancer antitumor Hedgehog pathway signaling Smoothened SMO Gli antagonist inhibitor receptor signal transduction biochemical gene regulation Hh protein regulator development cell-surface bind Patched activation GPCR-like vertebrate zinc-finger transcription factor family overactivation LDE225 NVPLDE225 antagonizing mouse human Gli1 mRNA expression tumor growth medulloblastoma allograft model phase II clinical trial treatment inhibit LDE 225

Product Overview:
Hedgehog (Hh) proteins, important regulators of development, bind the cell-surface protein Patched, allowing activation of the GPCR-like receptor, Smoothened (SMO).{21774} In vertebrates, this ultimately leads to the activation of the zinc-finger transcription factors of the Gli family. Overactivation of this pathway contributes to certain cancers.{27050} LDE225 is an Hh signaling pathway inhibitor that acts by antagonizing SMO (IC50s = 1.3 and 2.5 nM for mouse and human, respectively).{27243} A dose of 20 mg/kg/day LDE225 has been shown to penetrate the blood brain barrier, inhibit Gli1 mRNA expression, and prevent tumor growth in a medulloblastoma allograft mouse model.{27243} This compound has been investigated in phase II clinical trials for potential treatment of several Hh pathway activated cancers.

Size	1 mg
Shipping	dry ice
CAS Number	1218778-77-8
Molecular Formula	C₂₆H₂₆F₃N₃O₃ • 2H₃PO₄
SMILES	C[C@@H]1CN(C2=NC=C(NC(C3=CC=CC(C4=CC=C(OC(F)(F)F)C=C4)=C3C)=O)C=C2)C[C@H](C)O1.OP(O)(O)=O.OP(O)(O)=O
Molecular Weight	681,5
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.39
UNSPSC code	12352100

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MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

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