ALK-IN-1

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Chemical Structure| 1197958-12-5 同义名 : AP26113; Brigatinib analog; AP26113-analog
CAS号 : 1197958-12-5
货号 : A846689
分子式 : C26H34ClN6O2P
纯度 : 99%
分子量 : 529.01
MDL号 : MFCD23704187
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(94.52 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • mutant EGFR

    EGFR(del19), IC50:36.8 nM

    EGFR(C797S/del19), IC50:138.6 nM

  • ALK

    ALK, IC50:0.07 nM
描述 AP26113 is an analog of AP26113 which is a potent and selective ALK inhibitor. It is also an inhibitor of EGFR.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.89mL

0.38mL

0.19mL

9.45mL

1.89mL

0.95mL

18.90mL

3.78mL

1.89mL
参考文献

[1]Uchibori K, Inase N, et al. Brigatinib combined with anti-EGFR antibody overcomes osimertinib resistance in EGFR-mutated non-small-cell lung cancer. Nat Commun. 2017 Mar 13;8:14768.

[2]Huang WS, Liu S, et al.Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem. 2016 May 26;59(10):4948-64.