L LOXO-101(sulfat)

商品名稱 
分子式 C21H24F2N6O6S
分子量 526.51400
LogP 3.45140
PSA 168.98000
產(chǎn)品描述:loxo-101 is a small molecule that was designed to block the atp binding site of the trk family of receptors, with 2 to 20 nm cellular potency against the trka, trkb, and trkc kinases. \ ic50 value: 2 - 20 nm\ target: trka/b/c\ in vitro: loxo-101 is an orally administered inhibitor of the trk kinase and is highly selective only for the trk family of receptors. loxo-101 is evaluated for off-target kinase enzyme inhibition against a panel of 226 non-trk kinases at a compound concetion of 1,000 nm and atp concetinear the km for each enzyme. in the panel, loxo-101 demtrates greater than 50% inhibition for only one non-trk kinase (tnk2 ic50, 576 nm). measurement of proliferation following treatment with loxo-101 demtrates a dose-dependent inhibition of cell proliferation in all three cell lines. the ic50 is less than 100 nm for cuto-3.29 and less than 10 nm for km12 and mo-91, cistent with the known potency of this drug for the trk kinase family. [1] loxo-101 demtrtes potent and highly-selective inhibition of trka, trkb, and trkc over other kinase- and non-kinase targets. loxo-101 is a potent, atp-competitive trk inhibitor with ic50s in low nanomolar range for inhibition of all trk family members in binding and cellular assays, with 100x selectivity over other kinases. [2]\ in vivo: athymic nude mice injected with km12 cells are treated with loxo-101 orally daily for 2 weeks. dose-dependent tumor inhibition is observed, demtrating the ability of this selective compound to inhibit tumor growth in vivo. [1]