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LDE225 (NVP-LDE225,Erismodegib)

Cat No.
CEI-1393
Description
LDE225 is a potent and selective antagonist of Smoothened (Smo) with IC50 values of 2.5 nM and 1.3 nM for human Hedgehog and mouseHedgehog, respectively.
Product Overview
LDE225 is a potent and selective inhibitor of smoothened with IC50 values of 1.3nM in mouse and 2.5nM in human, respectively. LDE225 is screened out from a high-throughput cell-based screen of in-house diversity combinatorial libraries and is developed to be an antagonist of Smo. Smo is an activator of the hedgehog(Hh) signaling pathway and aberrant activation links to tumorigenesis in several cancers. The antitumor efficacy of LDE225 has been evaluated in vivo. In the subcutaneous Ptch+/-p53-/-medulloblastoma allograft mouse model, LDE225 can significantly inhibit tumor growth at a dose of 5mg/kg/day. And in an orthotopic Ptch+/-p53-/-medulloblastoma allograft model, LDE225 is suggested to penetrate the blood-brain barrier in tumor-bearing animals and cause the tumor growth inhibition after 4 days of treatment. Additionally, the preclinical safety assays show that LDE225 has no genotoxicity and has good selectivity.
CAS No.
956697-53-3
Molecular Weight
485.5
Purity
0.9898
Storage
Store at-20°C
Targets
human Hedgehog; mouseHedgehog
IC50
2.5 nM; 1.3 nM
Molecular Formula
C26H26F3N3O3
Chemical Name
N-[6-[(2S,6R)-2,6-dimethylmorpholin-4-yl]pyridin-3-yl]-2-methyl-3-[4-(trifluoromethoxy)phenyl]benzamide
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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