Name: LDE225 (NVP-LDE225,Erismodegib)
Price: 188.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    LDE225 is a potent and selective inhibitor of smoothened with IC50 values of 1.3nM in mouse and 2.5nM in human, respectively [1].
    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 [1].
    
    [1] Shifeng Pan, Xu Wu, Jiqing Jiang, et al. Discovery of NVP-LDE225, a potent and selective smoothened antagonist. ACS Med. Chem. Lett. 2010, 1: 130–134.
- Properties
  - Alternative Name
    
    N-[6-[(2S,6R)-2,6-dimethylmorpholin-4-yl]pyridin-3-yl]-2-methyl-3-[4-(trifluoromethoxy)phenyl]benzamide
    
    CAS Number
    
    956697-53-3
    
    Molecular Formula
    
    C26H26F3N3O3
    
    Molecular Weight
    
    485.5
    
    Appearance
    
    A solid
    
    Purity
    
    98.98%
    
    Solubility
    
    ≥24.3 mg/mL in DMSO; insoluble in H2O; ≥23 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Kowolik CM, Lin M, et al. "Attenuation of hedgehog/GLI signaling by NT1721 extends survival in pancreatic cancer." J Exp Clin Cancer Res. 2019 Oct 28;38(1):431. PMID:31661013
    2. Coffman LG, Choi YJ, et al. "Human carcinoma-associated mesenchymal stem cells promote ovarian cancer chemotherapy resistance via a BMP4/HH signaling loop." Oncotarget. 2016 Feb 9;7(6):6916-32. PMID:26755648

LDE225 (NVP-LDE225,Erismodegib)

LDE225 (NVP-LDE225,Erismodegib)

Background

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