An Hh signaling pathway inhibitor that acts by antagonizing SMO (IC50s = 1.3 and 2.5 nM for mouse and human

LDE225 (phosphate) – 1 mg

Brand:
Cayman
CAS:
1218778-77-8
Storage:
-20
UN-No:
Non-Hazardous - /

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.  

 

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Description

An Hh signaling pathway inhibitor that acts by antagonizing SMO (IC50s = 1.3 and 2.5 nM for mouse and human, respectively); inhibits Gli1 mRNA expression and prevents tumor growth in a medulloblastoma allograft mouse model at 20 mg/kg/day

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

Synonyms:  Erismodegib|NVP-LDE225|Sonidegib

Molecular weight: 681.5

CAS: 1218778-77-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer|Cell Signaling|Hedgehog Signaling||Research Area|Cell Biology|Cell Signaling|Hedgehog Signaling

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