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AP26113 (Brigatinib)
AP26113 (Brigatinib) is an orally available, potent and selective second generation inhibitor of anaplastic lymphoma kinase (ALK), displaying activity against the both wild type ALK (IC50 = 0.62 nM; Ki = 0.09 nM) and L1196M mutant (Ki = 0.08 nM), with about five-fold greater potency compared with Crizotinib [IC50 (ALK) = 3.6 nM; Ki (ALK) = 0.69 nM; Ki (L1196) = 8.2 nM] (Ref. 1). It is also a potent inhibitor of T790M-mutant EGFR. AP26113 has been designated as the Breakthrough Therapy by FDA for the treatment of patients with ALK positive (ALK+) metastatic non-small cell lung cancer (NSCLC) who are resistant to Crizotinib. It has shown sustained anti-tumor activity in patients with ALK+ NSCLC, including patients with active brain metastases in ongoing phase I/II trials.
Catalog NO: CT-AP261
Synonym: Brigatinib
CAS NO: 1197953-54-0
Mol. Formula: C29H39ClN7O2P
MW: 583.3
** The authoritatively disclosed structure (Ref. 3). A recrystallized powder (picture attached), >99.5% pure (HPLC at 214 and 254 nm), + clean NMR, coming with an excellent quantitative elemental analysis. Bulk stock!! Same day shipping.