BDTX-189 是一种高效可口服的选择性EGFR和HER2变构突变抑制剂，具有抗癌活性。它对 EGFR、HER2、BLK 和 RIPK2 的KD值分别为 0.2、0.76、13 和 1.2 nM。

BDTX-189 is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations(KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively). BDTX-189 exhibits anticancer activity.

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.?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

2414572-47-5

C29H29ClN6O4

561.04

BDTX-189

DMSO:41.67 mg/mL (74.27 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years