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ML-18

Cat. No. M8912
ML-18 Structure
Size Price Availability Quantity
5mg USD 225  USD225 In stock
10mg USD 325  USD325 In stock
50mg USD 1200  USD1200 In stock
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Quality Control & Documentation
Biological Activity

ML-18 is Bombesin receptor subtype 3 (BRS-3) antagonist (IC50 = 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 100 nM BA1 to cause tyrosine phosphorylation of the EGFR and ERK in lung cancer cells.

Protocol (for reference only)
Cell Experiment
Cell lines NCI-H727 or NCI-H1299 cells
Preparation method 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.
Concentrations 0, 4.8, 16, 48 μM
Incubation time 2 days
Animal Experiment
Animal models
Formulation
Dosages
Administration
Chemical Information
Molecular Weight 569.65
Formula C32H35N5O5
CAS Number 1422269-30-4
Form Solid
Solubility (25°C) DMSO: ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Moody TW, et al. Peptides. ML-18 is a non-peptide bombesin receptor subtype-3 antagonist which inhibits lung cancer growth.

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Keywords: ML-18 supplier, Bombesin Receptor, inhibitors, activators


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