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Brigatinib
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Brigatinib
CAS No. : 1197953-54-0
MCE 站:Brigatinib
产品活性:Brigatinib (AP-26113) 是有效,选择性的 ALK 抑制剂,IC50 值为 0.6 nM。
研究领域:Protein Tyrosine Kinase/RTK
作用靶点:ALK
In Vitro: Brigatinib potently inhibits the in vitro kinase activity of ALK (IC50, 0.6 nM) and all five mutant variants tested, including G1202R (IC50, 0.6-6.6 nM). Brigatinib demonstrates a high degree of selectivity, only inhibiting 11 additional native or mutant kinases with IC50 <10 nM. These include ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR (L858R; IC50, 1.5-2.1 nM). Brigatinib exhibits more modest activity against EGFR with a T790M resistance mutation (L858R/T790M), native EGFR, IGF1R, and INSR (IC50, 29-160 nM) and does not inhibit MET (IC50 >1000 nM). In cellular assays, brigatinib inhibits ALK and ROS1 with IC50s of 14 and 18 nM, respectively. Brigatinib inhibits FLT3 and IGF-1R with about 11-fold lower potency (IC50, 148-158 nM) and inhibits mutant variants of FLT3 and EGFR with 15- to 35-fold lower potency (IC50, 211-489 nM). Brigatinib inhibits cell growth with GI50 values ranging from 503 to 2,387 nM in three ALK-negative ALCL and NSCLC cell lines. Brigatinib inhibits ALK activity and abrogates proliferation of ALK addicted neuroblastoma cell lines, with IC50 of 75.27 ± 8.89 nM. Brigatinib inhibits both the ALK-I1171N and the ALK-G1269A mutant receptors at 10 and 4 nM levels, respectively.
In Vivo: Brigatinib (10, 25, or 50 mg/kg once daily, p.o.) leads to a dose-dependent inhibition of tumor growth in ALK+ Karpas-299 (ALCL) and H2228 (NSCLC) xenograft mouse models. Brigatinib markedly enhances survival of mice bearing ALK+ brain tumors compared with PF-02341066. Brigatinib (10, 25, 50 mg/kg, p.o.) results in dose-dependent antitumor activity, with tumor regressions in a mouse model of NSCLC.
相关产品:Drug Repurposing Compound Library Plus | FDA-Approved Drug Library Plus | Bioactive Compound Library Plus | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | FDA-Approved Drug Library | Anti-Cancer Compound Library | Drug Repurposing Compound Library | Orally Active Compound Library | FDA Approved & Pharmacopeial Drug Library | Anti-Lung Cancer Compound Library | Drug-Induced Liver Injury (DILI) Compound Library | Targeted Therapy Drug Library | A 83-01 | AZD-3463 | ALK inhibitor 1 | X-376 | ALK inhibitor 2 | HG-14-10-04 | 6-Demethoxytangeretin | JH-VIII-157-02 | ALK/ROS1-IN-1 | F-1 | TGFβRI-IN-2 | TL13-110 | TL13-22 | Ensartinib | WY-135
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热门标签:AP-26113