1422269-30-4
1422269-30-4 structure
- Name: ML 18
- Chemical Name: ML-18
- CAS Number: 1422269-30-4
- Molecular Formula: C32H35N5O5
- Molecular Weight: 569.651
- Catalog: Signaling Pathways GPCR/G Protein Bombesin Receptor
- Create Date: 2018-07-08 16:22:39
- Modify Date: 2024-01-09 06:27:14
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ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM.
| Name | ML-18 |
|---|---|
| Synonyms |
(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)- |
| Description | ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM. |
|---|---|
| Related Catalog | |
| Target |
IC50: 4.8 μM (BRS-3)[1] |
| 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 |
| 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 | light yellow solid |
| Vapour Pressure | 0.0±3.0 mmHg at 25°C |
| Index of Refraction | 1.652 |
| Storage condition | -20℃ |