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抑制剂/激活剂

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凋亡与自噬

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Brigatinib 布格替尼; AP-26113

Brigatinib (AP-26113) 是有效，选择性的 ALK 抑制剂，IC50 值为 0.6 nM。

货号：
TK0479
规格：

1mg

2mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	1197953-54-0
生物活性	Brigatinib (AP-26113) is a highly potent and selective ALK inhibitor, with an IC50 of 0.6 nM.
分子式	C29H39ClN7O2P
分子量	584.09
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	Ethanol : 10 mg/mL (17.12 mM; Need ultrasonic and warming) DMSO : 2 mg/mL (3.42 mM; Need ultrasonic)
体内研究	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.
体外研究	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.
文献	•Cancer Discov. 2018 Jun;8(6):714-729. •Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. •Theranostics. 2019 Jul 9;9(17):4878-4892. •Pharmacol Res. 2018 Nov;137:47-55. •Cancers (Basel). 2022, 14(1), 151. •Transl Oncol. 2021 Jan;14(1):100887. •Spectrochim Acta A Mol Biomol Spectrosc. 2020 Nov 14;119210. •Clin Chim Acta. 2018 May;480:180-185. •RSC Adv. 2018 8:1182-1190. •ChemMedChem. 2017 Nov 22;12(22):1857-1865. •Fundam Clin Pharmacol. 2021 Feb 1. •Eur J Drug Metab Pharmacokinet. 2021 Jul 18;1-11.
纯度及产品资料	98%

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