Cas No.: | 1422269-30-4 |
Chemical Name: | (S)-3-(1H-indol-3-yl)-N-((1-(4-methoxyphenyl)cyclohexyl)methyl)-2-(3-(4-nitrophenyl)ureido)propanamide |
Synonyms: | ML18,ML-18,ML 18,BRS-3 antagonist,1422269-30-4 |
SMILES: | O=C(NC1=CC=C([N+]([O-])=O)C=C1)N[C@H](C(NCC2(C3=CC=C(OC)C=C3)CCCCC2)=O)CC4=CNC5=C4C=CC=C5 |
Formula: | C32H35N5O5 |
M.Wt: | 569.67 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM. |
In Vitro: | ML-18 inhibits specific 125I-BA1 (DTyr-Gln-Trp-Ala-Val-βAla-His-Phe-Nle-NH2)BB6-14 binding to NCI-H1299 lung cancer cells stably transfected with BRS-3 with IC50 values of 4.8 μM. ML-18 binds with lower affinity to the GRPR and NMBR with IC50 values of 16 and more than 100 μM, respectively. ML-18 at 16 μM inhibits the ability of 10 nM BA1 to elevate cytosolic Ca2+ in a reversible manner using lung cancer cells loaded with FURA2-AM. ML-18 at 16 μM inhibits the ability of 100 nM BA1 to cause tyrosine phosphorylation of the EGFR and ERK in lung cancer cells. It inhibits the proliferation of lung cancer cells[1]. |