Mobocertinib succinate |
رقم الكتالوجGC62160 |
Mobocertinib (TAK-788) سكسينات هو مثبط EGFR / HER2 نشط عن طريق الفم ولا رجعة فيهMobocertinib succinate يثبط بشكل فعال المتغيرات السرطانية التي تحتوي على تنشيط طفرات EGFRex20ins مع انتقائية على EGFR من النوع البرييمكن استخدام Mobocertinib succinate في أبحاث NSCLC
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Cas No.: 2389149-74-8
Sample solution is provided at 25 µL, 10mM.
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.
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