Mobocertinib succinate (TAK-788 succinate) 是一种有效的的，具有口服活性的 EGFR 和 HER2 突变的抑制剂，包括外显子 20 的插入，并且选择性高于 WT EGFR。具有抗肿瘤活性。
货号:ajcx33172
CAS:2389149-74-8
分子式:C36H45N7O8
分子量：703.78
溶解度:DMSO : 25 mg/mL (35.52 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Mobocertinib succinate (TAK-788 succinate) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity[1][2].

Mobocertinib succinate (TAK-788 succinate) inhibits all 14 mutant variants of EGFR (IC50s=2.4-22 nM), and all 6 mutant variants of HER2 (IC50s=2.4-26 nM), more potently than it inhibited WT EGFR (IC50=35 nM), including all 8 variants with exon 20 activating insertions[1].

In mice implanted with a patient-derived tumor containing an EGFR exon 20 activating insertion, or with engineered Ba/F3 cells containing a HER2 exon 20 activating insertion, once daily oral dosing of Mobocertinib succinate induced regression of tumors at doses that were well tolerated (30-100 mg/kg)[1].

[1]. Francois Gonzalvez, et al. Abstract 2644: AP32788, a potent, selective inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, in preclinical models. April 16-20, 2016; New Orleans, LA.
[2]. Masood A, et al. Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in non-small cell lung cancer harboring uncommon EGFR mutations: Focus on BIBW 2992. Semin Oncol. 2019 Jun;46(3):271-283.