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LDE225, 2 mg

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Smoothened antagonist, inhibits Hedgehog signaling
SKU: ST10031
$125.00
 

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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
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

ST10031 Technical Data Sheet

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