Contact Us marketing@medicilon.com
CN
×
Close Button
Customer Center
Customer Center

A new LC-MS/MS method for the simultaneous quantification of Dabrafenib and its main metabolite hydroxy-dabrafenib (OHD) in human plasma has been developed and validated

2023-07-11
|
Page View:

14.jpgIncreased understanding of molecular pathways leads to the development of effective targeted therapies for the treatment of solid tumors. Dabrafenib (DAB) undergoes oxidative metabolism via cytochrome P450 (CYP) 3A4 and CYP2C8 to form hydroxy-dabrafenib (OHD), an active metabolite, with a twofold higher potency than an inhibitor of mutant BRAF. OHD (purity>99 %) was synthesized by Medicilon. Medicilon synthetic chemistry team is capable of the independent design of synthesis pathways and complex compound treatments, key to helping accelerate drug discovery.

Reference:

David Balakirouchenane, et al. Simultaneous quantification of dabrafenib, hydroxy-dabrafenib and trametinib in human plasma by liquid chromatography-tandem mass spectrometry. J Pharm Biomed Anal. 2021 Jan 30;193:113718. doi: 10.1016/j.jpba.2020.113718. 


Return
Relevant News
Researchers designed and synthesized a photocaged PI3K inhibitor 1, which could be readily activated by UV irradiation to release a highly potent PI3K inhibitor 2. ADME studies were conducted by Medicilon
2023-07-11
Aberrant activation of the PI3K pathway has been intensively targeted for cancer therapeutics for decades. In this work, researchers designed and synthesized a novel photocaged PI3K inhibitor 1, which could be readily activated by UV irradiation to release a highly potent PI3K inhibitor 2. ADME studies of compounds 1 and 2 were conducted by Medicilon. Medicilon's pharmacokinetics department offers the clients a broad spectrum of high quality of services in the areas of in vitro ADME, in vivo pharmacokinetics and bioanalysis services, ranging from small molecules to large molecules, such as protein and antibody.
Targeted protein degradation exemplified by PROTACs is an emerging strategy for drug discovery
2023-07-11
Targeted protein degradation (TPD) exemplified by PROTACs is an emerging strategy for next generation drug discovery. Threonine tyrosine kinase (TTK) is a dual-specific protein kinase that catalyzes phosphorylation of both serine/threonine and tyrosine residues. Researchers designed and synthesized TTK PROTACs, which demonstrated reasonable pharmacokinetic profiles. All the pharmacokinetic studies were carried out by Medicilon, according to the protocols and guidelines of the institutional care and use committee.
GS-5801 is a potent KDM5 inhibitor with antiviral activity against HBV. GS-5801 was synthesized by Medicilon
2023-07-11
​Chronic Hepatitis B virus is one of the main causes of liver diseases including cirrhosis and hepatocellular carcinoma. Isonicotinic acid inhibitors of the histone lysine demethylase 5 (KDM5) with potent anti-HBV activity. GS-5801, a potent inhibitor of KDM5, has antiviral activity against HBV in a primary human hepatocytes infection model, with the cellular permeability, oral bioavailability. GS-5801 was synthesized by Medicilon.