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ALK 抑制剂
LDK378 (Ceritinib) dihydrochloride是有效的抗ALK抑制剂,IC50为0.2 nM,对IGF-1R和InsR的选择性分别为40倍和35倍。
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c-Met/NPM-ALK 抑制剂
Crizotinib hydrochloride是c-Met激酶和NPM-ALK的抑制剂。
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- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
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ALK/MET inhibitor
Ensartinib hydrochloride (X-396 hydrochloride) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.
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ALK inhibitor
Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively.
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