ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM.
体外研究
ML-18 inhibits specific I-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 Ca 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.
分子式
C32H35N5O5
分子量
569.65
CAS号
1422269-30-4
运输条件
Room temperature in continental US; may vary elsewhere.