Agerafenib


Agerafenib is a selective multi-kinase inhibitor. It is undergoing a trial to test its ability to treat malignant tumors in humans. It is effective in doses ranging between 30 milligrams and 100 milligrams. It is also known as CEP-32496 and RXDX 105. It is a strong inhibitor of the BRAF gene, which is commonly found in cancerous cells.

Discovery

Agerafenib was originally discovered by a company called Daiichi Sankyo and Teva Pharmaceuticals during a research program. The chemical was originally named "CEP-32496" before being renamed to "RXDX 105" in 2015. It is currently undergoing a clinical trial to test its effectiveness against cancer in humans.

Characteristics

Agerafenib's chemical formula consists of 24 carbon atoms, 22 hydrogen atoms, 3 fluorine atoms, 5 nitrogen atoms and 5 oxygen atoms. The chemical's molar mass is 517.465 g/mol, and the monoisotopic mass is 517.157303 g/mol. It appears as a white to off-white crystalline powder in room temperature. Agerafenib has 5 hydrogen bond acceptors and 2 hydrogen bond donors. It has an partition coefficient of 4.35. It has 10 rotatable bonds and a topological polar surface area of 120.63.
The chemical is a strong inhibitor of the BRAF gene, which is present in around 7% of all malignant tumors. It does this due to its strong cytotoxicity to cells containing it. Agerafenib also inhibits phosphorylation in mitogen-activated protein kinase. The drug is shown to be most effective in humans in doses between 30 milligrams and 100 milligrams.