LDE225 (Erismodegib)

保质期 ：2 years

英文名 ：LDE225 (Erismodegib)

库存 ：10

供应商 ：上海伟进生物科技有限公司

CAS号 ：956697-53-3

保存条件 ：-20℃

规格 ：5mg

Biological Activity

LDE225 (Erismodegib) is an orally bioavailable, potent and specific small molecular antagonist of Hh pathway via the inhibition of Smoothened receptor (Smo). LDE225 binds to human and mouse Smo with high affinity (IC₅₀ ~11 nM), exceeding the potency of cyclopamine by a factor of > 20-fold. LDE225 dose-dependently inhibits Hh-Ag 1.5-induced basaloid tumor nests in embryonic or neonatal skin punches from Ptch1±heterozygous knock-out mice (IC₅₀ <150 nM). LDE225 also induces regression of preformed basaloid lesions (IC₅₀ <150 nM) and almost complete regression at 1.5 µM ^[1-2]. A phase I study of LDE225 for the treatment of patient with advanced solid tumors shows that it is well tolerated and has a favorable PK profile ^[3]. LDE225 also exhibits significant antitumor activities in preclinical mice models of islet cell neoplasms ^[4] and prostate cancer ^[5].

Chemical Properties

Cas No.: 956697-53-3	M. Wt.: 485.5
Formula: C26H26F3N3O3	Purity: ≥98%
Synonym: LDE-225, NVP-LDE225, Erismodegib
Chemical Name: N-(6-((2S,6R)-2,6-dimethylmorpholino)pyridin-3-yl)-2-methyl-4′-(trifluoromethoxy)biphenyl-3-carboxamide
Solubility: Soluble in DMSO up to 100 mM. Very sparingly soluble in water.
Storage: Store powder at -20 ºC for the stability of two years.