Brigatinib

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Brigatinib

CAS No. : 1197953-54-0

MCE 国际站：Brigatinib

产品活性：Brigatinib (AP-26113) 是一种有效，选择性的，具有口服活性的 ALK 抑制剂，IC₅₀ 值为 0.6 nM。Brigatinib 可用于非小细胞肺癌 (NSCLC) 的研究。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Anaplastic lymphoma kinase (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.

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