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ML-18
🥰Excellent
Catalog No. T4540Cas No. 1422269-30-4
ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 [mu]M.
ML-18
🥰Excellent
Purity: 100%
Catalog No. T4540Cas No. 1422269-30-4
ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 [mu]M.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $30 | In Stock | |
| 5 mg | $58 | In Stock | |
| 10 mg | $93 | In Stock | |
| 25 mg | $188 | In Stock | |
| 50 mg | $293 | In Stock | |
| 100 mg | $473 | In Stock | |
| 200 mg | $653 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $73 | In Stock |
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Purity:100%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 [mu]M. |
| Targets&IC50 | BRS3:4.8 μM. |
| In vitro | ML-18, at a concentration of 16 µM, reversibly inhibits BA1 at 10 nM from increasing cytosolic Ca2+ levels and at 100 nM from inducing tyrosine phosphorylation of EGFR and ERK in lung cancer cells, using FURA2-AM-loaded lung cancer cells for the former evaluation. This compound also suppresses lung cancer cell proliferation. Furthermore, ML-18 demonstrates specific inhibition of 125I-BA1 (DTyr-Gln-Trp-Ala-Val-βAla-His-Phe-Nle-NH2)BB6-14 binding to BRS-3-expressing NCI-H1299 lung cancer cells, presenting an IC50 value of 4.8 µM. It exhibits reduced affinity towards GRPR and NMBR with IC50 values of 16 µM and over 100 µM, respectively. |
| 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. |
| Cell Research | ML-18 is dissolved in DMSO at a concentration of 10 mM prior to use. 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. |
| Molecular Weight | 569.65 |
| Formula | C32H35N5O5 |
| Cas No. | 1422269-30-4 |
| Smiles | COc1ccc(cc1)C1(CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)Nc2ccc(cc2)[N+]([O-])=O)CCCCC1 |
| Relative Density. | 1.291 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (87.77 mM)  | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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