BDTX-189 (Synonyms: BDTX-189) |
| رقم الكتالوجGC60629 |
BDTX-189 (BDTX-189) هو مثبط فعال وانتقائي فموياً للطفرات الورمية الخيفية EGFR و HER2 ، بما في ذلك طفرات الإدراج EGFR / HER2 exon 20. يُظهر BDTX-189 KDs 0.2 و 0.76 و 13 و 1.2 نانومتر لـ EGFR و HER2 و BLK و RIPK2 ، بشكل حصاد. نشاط مضاد للسرطان.
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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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