生物活性 | |||
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描述 | Larotrectinib (LOXO-101) is an ATP-competitive oral inhibitor targeting the tropomyosin-related kinase (TRK) family of receptor kinases (TRKA, B, and C). It exhibits low nanomolar 50% inhibitory concentrations against all three isoforms and demonstrates 1,000-fold or greater selectivity relative to other kinases[1][2]. Assessment of cell proliferation post-treatment with Larotrectinib (LOXO-101) reveals a dose-dependent suppression across all three cell lines. The IC50 values are below 100 nM for CUTO-3.29 and below 10 nM for KM12 and MO-91, aligning with the established potency of this drug against the TRK kinase family[3]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.33mL 0.47mL 0.23mL |
11.67mL 2.33mL 1.17mL |
23.34mL 4.67mL 2.33mL |