M-475271 (AZM475271) is an investigational drug targeting cancer invasion and metastasis. It is an aminoquinoline class inhibitor with high affinity and specificity for the nonreceptor tyrosine kinase (Src). In vitro AZM475271 demonstrated strong dose-dependent inhibition of Src tyrosine kinase activity in the L3.6pl human pancreatic carcinoma cell line. The IC50 concentration of AZM475271 to inhibit the phosphorylation of c-Src, lck, and c-yes was 0.01, 0.03, and 0.08 uM, respectively, in comparison with an IC50 of 0.7 uM AZM475271 to inhibit KDR. AZM475271 reduced tumor size, vascularity and metastasis, and increased apoptosis in human pancreatic cells grown orthotopically in nude mice. It also exhibited antiangiogenic activity in vitro and in vivo, and sensitized tumor cells to the cytotoxic effects of gemcitabine. The effect of daily oral treatment with M475271 on subcutaneous tumors and lung metastasis caused by human lung adenocarcinoma cells in NK-cell depleted SCID mice demonstrated inhibition of the growth of subcutaneous tumors via inhibition of tumor cells proliferation, VEGF production and/or vascularization in the mice in a dose-dependent manner. In the metastasis model with A549 cells, the lung weight in the M475271 (50 mg/kg)-treated group was less than that of the control group, despite no difference in the number of metastatic nodules. These findings suggest that M475271 may be efficacious in treating pancreatic adenocarcinomas and might be helpful for controlling the progression of human lung adenocarcinomas.

Fluvastatin Anti-Isomer is a metabolite of lipid-lowering agent Fluvastatin. Fluvastatin is very unstable during storage and anti-isomer as well as lactones are the main formed by-products.

4-Nitro-3-trifluoromethylaniline is one of the two main products of flutamide metabolism in human liver microsomes. Also, it is a major urinary metabolite of S-1 [3-(4-fluorophenoxy)-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]-propanamide] - a member of a series of potent selective androgen receptor modulators.

UNC-0638, an inhibitor of G9a and GLP with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets. UNC-0638 treatment of a variety of cell lines resulted in lower global H3K9me2 levels, equivalent to levels observed for small hairpin RNA knockdown of G9a and GLP with the functional potency of UNC-0638 being well separated from its toxicity. UNC0638 markedly reduced the clonogenicity of MCF7 cells, reduced the abundance of H3K9me2 marks at promoters of known G9a-regulated endogenous genes and disproportionately affected several genomic loci encoding microRNAs. In mouse embryonic stem cells, UNC-0638 reactivated G9a-silenced genes and a retroviral reporter gene in a concentration-dependent manner without promoting differentiation. UNC-0638 is not suitable for animal studies due to its poor pharmacokinetic (PK) properties.

Nervonic acid is a long chain unsaturated fatty acid that is enriched in sphingomyelin. It consists of choline, sphingosine, phosphoric acid, and fatty acid. Nervonic acid may enhance the brain functions and prevent demyelination (Chemical Land21). Research shows that there is negative relationship between nervonic acid and obesity-related risk factors. Demyelination in adrenoleukodystrophy (ALD) is associated with an accumulation of very long chain saturated fatty acids stemming from a genetic defect in the peroxisomal beta oxidation system responsible for the chain shortening of these fatty acids. Sphingolipids from post mortem ALD brain have decreased levels of nervonic acid, 24:1(n-9), and increased levels of stearic acid, 18:0. Nervonic acid (C24:1), a component of membrane sphingolipids and phosphatidylethanolamines, may be a useful predictor of chronic kidney disease mortality and diabetes. Nervonic acid oils are being studied for pharmaceutical, nutraceutical and industrial applications. Nervonic acid is a major component of Lunaria oil. There is increasing evidence that dietary supplementation with nervonic acid is healthy for babies and infants during the early stage of brain development. Nervonic acid has been reported to reduce the shaking associated with Parkinson’s disease and the numbness caused by multiple sclerosis. It also has potential for treating schizophrenia and reducing early Alzheimer’s symptoms.