Avapritinib-d3 is a deuterium-labeled derivative of Avapritinib, a potent and selective inhibitor of mutant kinase targets KIT and PDGFRA. It demonstrates remarkable biological activity with IC50 values of 0.27 nM and 0.24 nM for KIT D816V and PDGFRA D842V mutations, respectively. Avapritinib-d3 binds to the active conformation of these kinases, contributing to its antitumor effects, and it also inhibits the transport functions of ABCB1 and ABCG2. This stable isotope variant is useful for pharmacokinetic studies and tracer applications in chemical research.
Avapritinib-d3 is a deuterium-labeled derivative of Avapritinib, a potent and selective inhibitor of mutant kinase targets KIT and PDGFRA. It demonstrates remarkable biological activity with IC50 values of 0.27 nM and 0.24 nM for KIT D816V and PDGFRA D842V mutations, respectively. Avapritinib-d3 binds to the active conformation of these kinases, contributing to its antitumor effects, and it also inhibits the transport functions of ABCB1 and ABCG2. This stable isotope variant is useful for pharmacokinetic studies and tracer applications in chemical research.
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