BDTX-189 (Synonyms: BDTX-189) |
| Catalog No.GC60629 |
Le BDTX-189 (BDTX-189) est un inhibiteur puissant, actif par voie orale et sélectif des mutations oncogènes allostériques de l'EGFR et de HER2, y compris les mutants d'insertion de l'exon 20 de l'EGFR/HER2. BDTX-189 montre des KD de 0,2, 0,76, 13 et 1,2 nM pour EGFR, HER2, BLK et RIPK2, respectivement. Activité anticancéreuse.
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Cas No.: 2414572-47-5
Sample solution is provided at 25 µL, 10mM.
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BDTX-189 is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, includes EGFR/HER2 exon 20 insertion mutants. BDTX-189 shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity[1].
BDTX-189 is a masterKey inhibitor of the ERBB allosteric mutant oncogene family with antiproliferative activity (IC50<100 nM for ERBB allosteric mutant oncogene family)[1].
BDTX-189 (0-100 mg/kg; p.o.; daily for 15 dyas) shows dose-dependent tumor growth inhibition and regression in in athymic nude mice bearing HER2 S310F Ba/F3 allograft tumors[1].BDTX-189 (1-50 mg/kg.p.o.; daily for 15 days) shows dose-dependent tumor growth inhibition and regression in athymic nude mice bearing CUTO-14 PDX tumors that express the EGFR mutation EGFR ASV[1].
[1]. Elizabeth Buck, et al. BDTX-189, a Potent and Selective Inhibitor of Allosteric EGFR and HER2 Oncogenic Mutations.
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