AP26113 (BRIGATINIB)

Catalog No.	APIM050078
Product Name	AP26113 (BRIGATINIB)

Description

Background Information:

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.

Reference:

1. Shaw, A. T.; et. al. Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc Natl Acad Sci U S A. 2011, 108(18), 7535-7540.
2. Gettinger, S.; et. al. 1292P Alk Inhibitor Ap26113 In Patients With Advanced Malignancies, Including Alk+ Non-Small Cell Lung Cancer (Nsclc): Updated Efficacy And Safety Data. Ann Oncol 2014, 25(suppl 4), iv455.
3. BUYER BEWARE: A wrong structure of AP26113 (Brigatinib) (with CAS No. 1197958-12-5, Molecular Formula: C26H34ClN6O2P, and Mol. Wt: 529.01) has been circulating for many years in marketplace by many other vendors (no exception). Regrettably, many papers have been published using the wrong structure. To date (02-01-2016), the wrong structure AP26113 is still being marketed by many.

APIM050078: AP26113 (BRIGATINIB)

CAS No.: 1197953-54-0.
Molecular Formula: C29H39ClN7O2P.
Molecular Weight: 583.3.
Purity: >99% by HPLC.
QC: HPLC-MS, NMR and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0-4 °C (short term), -20 °C (Long term), Desiccated.

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