UniPR1331

Cas No.:	1809170-59-9
Chemical Name:	((R)-4-((3S,8S,9S,10R,13R,14S,17R)-3-hydroxy-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentanoyl)-L-tryptophan
Synonyms:	UniPR-1331
SMILES:	C(O)(=O)[C@@H](CC1C2C(=CC=CC=2)NC=1)NC(=O)CC[C@@H]([C@H]1[C@@](C)2CC[C@]([H])3[C@@](C)4CC[C@@H](O)CC4=CC[C@]3([H])[C@@]2([H])CC1)C
Formula:	C35H48N2O4
M.Wt:	560.779
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

UniPR1331 (UniPR-1331) is a selective, orally available antagonist of Eph/ephrin interaction with pIC50 of 5.45, IC50 of 2.9 uM; demonstrates anti-angiogenic agent in endothelial cells, bioavailable in mice by the oral route and devoid of biological activity on G protein-coupled and nuclear receptors targeted by bile acid derivatives; blocks the tube formation of HBMVEC in a concentration-dependent manner with IC50 of 3.9 uM, dramatically inhibits vessel formation induced by VEGF165 in in vivo in the CAM assay, does not interfere with the kinase activity of VEGFR2; inhibits ephrin-A1 induced EphA2 phosphorylation decreasing EphA2 expression on U87MG cells, without interfering with the enzymatic activity of EphA2; prolongs survival in glioblastoma and potentiates the effect of antiangiogenic therapy in mice.