DBPR112 HCl - CAS 2889316-21-4

DBPR112 is a potent EGFR inhibitor (IC50=487 nM) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. DBPR112), DBPR112 not only displayed a potent inhibitory activity against EGFRL858R/T790M double mutations but also exhibited tenfold potency better than the third-generation inhibitor, osimertinib, against EGFR and HER2 exon 20 insertion mutations. Overall, pharmacokinetic improvement through lead-to-candidate optimization yielded fourfold oral AUC better that afatinib along with F = 41.5%, an encouraging safety profile, and significant antitumor efficacy in in vivo xenograft models.

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2889291

C32H32ClN5O3

570.08

N([C@H](CO)C1=CC=CC=C1)C2=C3C(=C(OC3=NC=N2)C4=CC=CC=C4)C5=CC(NC(/C=C/CN(C)C)=O)=CC=C5.Cl

-20°C

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Small Compound