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AZD3463 is a novel inhibitor of ALK which overcomes multiple mechanisms of acquired resistance to crizotinib. AZD3463 inhibits ALK with a Ki value of 0.75 nM. AZD3463 dose-dependently inhibits pALK in tumor xenografts in vivo, resulting in stasis (H3122) or regression (DEL, H2228) in tumor volume. AZD3463 obtains equivalent potency to mutantL1196M and wild-type ALK in vivo.
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Source | Sci Rep (2016). Figure 2. AZD3463 |
| Method | colony formation assay | |
| Cell Lines | NB cells | |
| Concentrations | 5 μM | |
| Incubation Time | 4 hrs | |
| Results | Our data indicates that AZD3463 effectively blocks both anchorage-dependent and independent colony formation of NB cells. |
| Molecular Weight | 448.95 |
| Formula | C24H25ClN6O |
| CAS Number | 1356962-20-3 |
| Solubility (25°C) | DMSO 20 mg/mL |
| 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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