SBI-0640756 is a first-in-class inhibitor that targets eIF4G1 and disrupts the eIF4F complex. SBI-0640756 impaired the eIF4F complex assembly independently of mTOR and attenuated growth of BRAF-resistant and BRAF-independent melanomas. SBI-0640756 (SBI-756) inhibits the growth of NRAS, BRAF, and NF1-mutant melanomas in vitro.
In vivo, SBI-0640756 (SBI-756) delays the onset and reduces the incidence of Nras/Ink4a melanomas.
|Cell lines||Melanoma lines|
|Preparation method||Melanoma lines are plated (triplicates 384-well plates; 1,500 cells per well) and cell viability is assessed 48 hours after treatment with indicated compounds. Growth inhibition is calculated as percentage of DMSO-treated controls and is plotted against the log drug concentration.|
|Concentrations||1, 2, 5 μmol/L|
|Incubation time||48 h|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 60 mg/mL|
SBI-0640756 Attenuates the Growth of Clinically Unresponsive Melanomas by Disrupting the eIF4F Translation Initiation Complex.
Feng Y, et al. Cancer Res. 2015 Dec 15;75(24):5211-8. PMID: 26603897.
|NADP disodium salt
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L-Glutamic acid monosodium salt hydrate is also a Kainate receptor, NMDA receptor and quisqualate receptor agonist; an excitatory amino acid neurotransmitter.
Lipopolysaccharides (LPS) is an endotoxin derived from the outer leaflet of the outer membrane of Gram-negative bacteria.
PEG6000 is a neutral and biocompatible hydrophilic polymer.
Hippuric acid is a low molecular weight phenolic carboxylic acid urinary metabolite that may be a useful urinary biomarker for certain cancers such as gastric cancer and oxidative stress.
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