NVP-LDE225|Smoothened (Smo) antagonist|DC Chemicals

NVP-LDE225|Smoothened (Smo) antagonist|DC Chemicals

LDE225 (NVP-LDE225) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively. Phase 3.

Product Name: NVP-LDE225(Erismodegib) |Catalog Number: DC8493 |CAS 956697-53-3 |Other names: NVP-LDE225,LDE225 |Chemical Name: [1,1'-Biphenyl]-3-carboxamide,N-[6-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-3-pyridinyl]-2-methyl-4'-(trifluoromethoxy)-,rel- |Molecule Formular: C26H26F3N3O3 |MW: 485.5

LDE225 inhibits TM3 luciferized cell line with 0.6 nM and 8 nM, at the presence of 1 nM and 25 nM Hh agonist Ag1.5, respectively. LDE225 is highly bound to mouse, rat, and human plasma proteins (>99%) and moderately bound to dog and monkey plasma proteins (77 and 85%, respectively). LDE225 has high permeability (90.8% in man) in the PAMPA assay. LDE225 shows good oral bioavailability ranging from 69 to 102% in preclinical species when dosed in solution. LDE225 is a weak base with a measured pKa of 4.20 and exhibits relatively poor aqueous solubility. LDE225 demonstrates dose-related antitumor activity. At a dose of 5 mg/kg/day qd, LDE225 significantly inhibits tumor growth, corresponding to a T/C value of 33%. When dosed at 10 and 20 mg/kg/day qd, LDE225 gives rise to 51 and 83% regression, respectively. Gli1 mRNA inhibition correlates with tumor and plasma exposure of LDE225. LDE225 successfully penetrates the blood−brain barrier in tumor-bearing animals and results in tumor growth inhibition after 4 days of treatment. [1] LDE225 significantly reduces the tumor volume by 95.7% in Rip1-Tag2 mice. LDE225 prolongs survival in Rip1Tag2 mice. LDE225 decreases expression of stromal markers in the LDE225-treated mice. [2]For the detailed information of NVP-LDE225, the solubility of NVP-LDE225 in water, the solubility of NVP-LDE225 in DMSO, the solubility of NVP-LDE225 in PBS buffer, the animal experiment (test) of  NVP-LDE225, the cell expriment (test) of NVP-LDE225, the in vivo, in vitro and clinical trial test of NVP-LDE225, the EC50, IC50,and Affinity of NVP-LDE225, Please contact DC Chemicals.

For research and scientific purpose only, not for human use.