BDTX-189是一种高效的具有口服活性的选择性EGFR、HER2变构突变抑制剂，包括EGFR/HER2外显子20插入突变。BDTX-189对EGFR、HER2、BLK和RIPK2的KD值分别显示0.2、0.76、13和1.2nM。具有抗癌活性。
货号:ajcx30248
CAS:2414572-47-5
分子式:C29H29ClN6O4
分子量：561.03
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.