ML 18
Names
[ CAS No. ]:
1422269-30-4
[ Name ]:
ML 18
[Synonym ]:
(1Z,2S)-2-[(E)-{Hydroxy[(4-nitrophenyl)amino]methylene}amino]-3-(1H-indol-3-yl)-N-{[1-(4-methoxyphenyl)cyclohexyl]methyl}propanimidic acid
1H-Indole-3-propanimidic acid, α-[[(1E)-hydroxy[(4-nitrophenyl)amino]methylene]amino]-N-[[1-(4-methoxyphenyl)cyclohexyl]methyl]-, (αS)-
Biological Activity
[Description]:
ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM.
[Related Catalog]:
[Target]
[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].
[Kinase Assay]
The cells are incubated in SIT buffer containing 0.25% bovine serum albumin and 250 μg/mL bacitracin and 125I-BA1 (100,000 cpm) is added, as well as various concentrations of unlabelled competitor (ML-18). After incubation at 37°C for 30 min, free 125I-BA1 is removed by washing 3 times in buffer and the cells which contain bound 125I-BA1 is dissolved in 0.2 N NaOH and counted in a gamma counter. The IC50 is calculated for each unlabeled competitor[1].
[Cell Assay]
Cell viability is measured using the MTT assay. NCI-H727 or NCI-H1299 cells transfected with BRS-3 are treated with ML-18 (0, 4.8, 16, 48 μM) or gefitinib added. After 2 days, 15 μL of 0.1 % MTT solution added. After 4 h, 150 μL of DMSO is added. After 16 h, the optical density at 570 nm is determined[1].
[References]
[Related Small Molecules]
Chemical & Physical Properties
[ Density]:
1.3±0.1 g/cm3
[ Boiling Point ]:
803.5±75.0 °C at 760 mmHg
[ Molecular Formula ]:
C32H35N5O5
[ Molecular Weight ]:
569.651
[ Flash Point ]:
439.7±37.1 °C
[ Exact Mass ]:
569.263794
[ LogP ]:
8.03
[ Appearance of Characters ]:
light yellow solid
[ Vapour Pressure ]:
0.0±3.0 mmHg at 25°C
[ Index of Refraction ]:
1.652
[ Storage condition ]:
-20℃