Description
Details
LDE225 is a potent and specific Hedgehog pathway inhibitor through binding and antagonizing Smoothened (IC50 = 11 nM). LDE225 has been shown to induce tumor regression in animal models of medulloblastoma. It is currently in the clinical trials to treat cancers.
Details
Details
Molecular Weight | 485.5 |
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Molecular Formula | C26H26F3N3O3 |
Chemical Name | N-(6-[(2R,6S)-2,6-dimethylmorpholin-4-yl]pyridin-3-yl)-2-methyl-3-[4-(trifluoromethoxy)phenyl]benzamide |
CAS Number | 956697-53-3 |
PubChem Identifier | 24775005 |
Appearance | White to off-white solid |
Purity | >98% by HPLC analysis |
Alternative Names | Erismodegib, NVP-LDE225 |
Solubility | Soluble in DMSO at 100 mM |
Reconstitution | For a 10 mM concentrated stock solution, reconstitute the compound by adding 412 μL of DMSO to the entire contents of vial. If precipitate is observed, warm the solution to 37°C for 2 to 5 minutes. |
Storage and Stability | Solid: Shipped at room temperature. Store at -20°C. Stable for 6 months when stored as directed. Solution: Following reconstitution, store aliquots in tightly sealed vials at -20°C. Avoid repeated freeze-thaw cycles. |
References | Buonamici, S., et al. (2010) Interfering with resistance to smoothened antagonists by inhibition of the PI3K pathway in medulloblastoma. Sci Transl Med 2(51): 51. PMID: 20881279. Heller, E., et al. (2012) Hedgehog signaling inhibition blocks growth of resistant tumors through effects on tumor microenvironment. Cancer Res 72(4): 897-907. PMID: 22186138. Pan, S., et al. (2010) Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist. ACS Med Chem Lett 1(3): 130-134. PMID: 24900187. |
Technical Documents |