Mobocertinib succinate |
| Katalog-Nr.GC62160 |
Mobocertinib (TAK-788) Succinat ist ein oral aktiver und irreversibler EGFR/HER2-Hemmer. Mobocertinibsuccinat hemmt wirksam onkogene Varianten, die aktivierende EGFRex20ins-Mutationen mit SelektivitÄt gegenÜber Wildtyp-EGFR enthalten. Mobocertinibsuccinat kann in der NSCLC-Forschung eingesetzt werden.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2389149-74-8
Sample solution is provided at 25 µL, 10mM.
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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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