NVP-LDE225 Chemical Properties

Melting point:

154-157°C

Boiling point:

544.5±50.0 °C(Predicted)

Density 

1.255

storage temp. 

Refrigerator

solubility 

DMSO (Slightly), Methanol (Slightly)

form 

White solid.

pka

9.53±0.70(Predicted)

color 

Light Purple

Safety Information

HS Code 

2934999090

NVP-LDE225 Usage And Synthesis

Uses

A potent, selective and orally bioavailable Smoothened (SMO) antagonist; it inhibits hedgehog (Hh) signaling pathway via antagonism of the Smoothened receptor (SMO). Antineoplastic. Potent Hedgehog inhibitor.

Definition

ChEBI: A member of the classo of biphenyls that is the amide obtained by formal condensation of the carboxy group of 2-methyl-4'-(trifluoromethoxy)[1,1'-biphenyl]-3-carboxylic acid with the amino group of 6-(2,6-dimethylmorpholin-4-yl)pyridin-3-amine. Used (as it phosphate salt) for treatment of locally advanced basal cell carcinoma.

Biological Activity

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].

target

human Hedgehog

storage

Store at -20°C

References

[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.

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