BLZ945 - CAS 953769-46-5
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Not Intended for Therapeutic Use. For research use only.
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BLZ945 is an orally active, potent and selective CSF-1R inhibitor, which inhibits CSF-1R activity with an IC50 of 1nM and is more than 1000-fold selective against its closest receptor tyrosine kinase homologs c-KIT and Platelet-derived Growth Factor Receptor beta (PDGFRb).
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1.Phenotypic and metabolic investigation of a CSF-1R kinase receptor inhibitor (BLZ945) and its pharmacologically active metabolite.
Krauser JA1, Jin Y, Walles M, Pfaar U, Sutton J, Wiesmann M, Graf D, Pflimlin-Fritschy V, Wolf T, Camenisch G, Swart P. Xenobiotica. 2015 Feb;45(2):107-23. doi: 10.3109/00498254.2014.945988. Epub 2014 Sep 2.
1. 4-[2((1R,2R)-2-Hydroxycyclohexylamino)-benzothiazol-6-yloxyl]-pyridine-2-carboxylic acid methylamide (BLZ945) is a small molecule inhibitor of CSF-1R kinase activity within osteoclasts designed to prevent skeletal related events in metastatic disease. Key metabolites were enzymatically and structurally characterized to understand the metabolic fate of BLZ945 and pharmacological implications. The relative intrinsic clearances for metabolites were derived from in vitro studies using human hepatocytes, microsomes and phenotyped with recombinant P450 enzymes. 2. Formation of a pharmacologically active metabolite (M9) was observed in human hepatocytes. The M9 metabolite is a structural isomer (diastereomer) of BLZ945 and is about 4-fold less potent. This isomer was enzymatically formed via P450 oxidation of the BLZ945 hydroxyl group, followed by aldo-keto reduction to the alcohol (M9). 3. Two reaction phenotyping approaches based on fractional clearances were applied to BLZ945 using hepatocytes and liver microsomes.
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CAS 953769-46-5 BLZ945

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