Phone: 1-617-401-8149
Fax: 1-617-606-5019
Email: message@sydlabs.com
Or leave a message with a formal purchase
order (PO) Or credit card.
| Catalog No. | Product Name | Size | List Price (US$) | Quantity |
|---|
Price/availability/specifications subject to change without notice. Unless otherwise indicated, our catalog and customized products are for research use only and not intended for human or animal diagnostic or therapeutic use.
Phone: 1-617-401-8149
Fax: 1-617-606-5019
Email: message@sydlabs.com
Or leave a message with a formal purchase
order (PO) Or credit card.
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.
Copyright © 2009-2022 sydlabs.com. All rights reserved.
Use of this website means that you have read, understood, and accepted the Syd Labs Privacy Policy and Terms & Conditions.