Product Name:

CH-5424802 (RG-7853, AF-802)

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CAT#: A-1176    

Chemical Structure
CH-5424802 structure

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Related ALK Inhibitors

Biological Activity

CH-5424802 (RG-7853, AF-802) is a potent and selective ALK inhibitor
Technical Data

Synonyms: 9-Ethyl-6,11-dihydro-6,6-dimethyl-8-[4-(4-morpholinyl)-1-piperidinyl]-11-oxo-5H-benzo[b]carbazole-3-carbonitrile;
Molecular Formula: C30H34N4O2
Purity: >99%
Storage Conditions: 2ºC to 8 ºC, or -20ºC for 2 years.
CH-5424802 MSDS CH-5424802 CoA
9-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
Anaplastic 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.