NVP-LDE225

Bezeichnung:NVP-LDE225

CAS-Nr956697-53-3

Englisch Name:NVP-LDE225

CBNumberCB52515129

SummenformelC26H26F3N3O3

Molgewicht485.5

MOL-Datei956697-53-3.mol

NVP-LDE225 physikalisch-chemischer Eigenschaften

Schmelzpunkt	154-157°C
Siedepunkt	544.5±50.0 °C(Predicted)
Dichte	1.255
storage temp.	Refrigerator
Löslichkeit	DMSO (Slightly), Methanol (Slightly)
Aggregatzustand	White solid.
pka	9.53±0.70(Predicted)
Farbe	Light Purple

Sicherheit

HS Code

2934999090

Gefahreninformationscode (GHS)

NVP-LDE225 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
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.
Biologische Aktivität
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
Lager
Store at -20°C
Einzelnachweise
[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.

NVP-LDE225 Upstream-Materialien And Downstream Produkte

NVP-LDE225 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Send Inquriy