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CH5424802 (AF802) is a potent, selective, and orally available ALK inhibitor. Anaplastic lymphoma kinase (ALK) receptor tyrosine kinase is considered an attractive therapeutic target for human cancers. CH5424802 (AF802) 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. CH5424802 inhibited ALK L1196M, which corresponds to the gatekeeper mutation conferring common resistance to kinase inhibitors. CH5424802 also blocked EML4-ALK L1196M-driven cell growth.
| Molecular Weight | 519.08 |
| Formula | C30H35ClN4O2 |
| CAS Number | 1256589-74-8 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related ALK Products |
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| F-1
F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50 values of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively. |
| TL13-22
TL13-22 is a negative control for TL13-12 and a potent ALK inhibitor with an IC50 of 0.54 nM. |
| TL13-110
TL13-110 is a negative control for TL13-112 and a potent ALK inhibitor with an IC50 of 0.34 nM. |
| ALK inhibitor 2
ALK inhibitor 2 is a potent pyrimidin ALK inhibitor. |
| NVL-655 TFA
NVL-655 (ALK-IN-27) TFA is a novel, brain-permeable, selective ALK inhibitor with antitumor activity. For Ba/F3 CLIP1-LTK cells, NVL-655 (ALK-IN-27) TFA has an IC50 of 2.7 nM. It can be used in studies related to ALK-positive non-small cell lung cancer (NSCLC). |
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