CH-5424802 (RG-7853, AF-802)Request CH-5424802
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Related ALK Inhibitors
CH-5424802 (RG-7853, AF-802) is a potent and selective ALK inhibitor
Molecular Formula: C30H34N4O2
M.Wt.:482.62 CAS#:1256580-46-7 Purity: >99%
Storage Conditions: 2ºC to 8 ºC, or -20ºC for 2 years.
CH-5424802 MSDS CH-5424802 CoA
Reference9-Substituted 6, 6-Dimethyl-11-oxo-6, 11-dihydro-5H-benzo [b] carbazoles as Highly Selective and Potent Anaplastic Lymphoma Kinase Inhibitors
K Kinoshita, T Kobayashi, K Asohˇ - Journal of Medicinal ˇ, 2011 - ACS Publications... intermediate 12. Recently, we obtained an X-ray cocrystal structure of another 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazole derivative 14 (CH-5424802 (RG-7853, AF-802), Figure 2)(23) with human ALK (PDB code 3AOX). The binding ...
CH-5424802 (RG-7853, AF-802), a Selective ALK Inhibitor Capable of Blocking the Resistant Gatekeeper Mutant
www.cell.com/cancer-cell/abstract/S1535-6108(11)00148-6Anaplastic lymphoma kinase (ALK) is a tyrosine kinase that is constitutively activated in certain cancers, following gene alterations such as chromosomal translocation, amplification, or point mutation. Here, we identified CH-5424802 (RG-7853, AF-802), a potent, selective, and orally available ALK inhibitor with a unique chemical scaffold, showing preferential antitumor activity against cancers with gene alterations of ALK, such as nonsmall cell lung cancer (NSCLC) cells expressing EML4-ALK fusion and anaplastic large-cell lymphoma (ALCL) cells expressing NPM-ALK fusion in vitro and in vivo. CH-5424802 (RG-7853, AF-802) inhibited ALK L1196M, which corresponds to the gatekeeper mutation conferring common resistance to kinase inhibitors, and blocked EML4-ALK L1196M-driven cell growth. Our results support the potential for clinical evaluation of CH-5424802 (RG-7853, AF-802) for the treatment of patients with ALK-driven tumors.