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X-376 is a potent and highly specific ALK small molecule tyrosine kinase inhibitors (TKIs) with IC50 of 0.61 nM. In Ambit kinome screens, cell growth inhibition studies, and surrogate kinase assays, X-376 was more potent inhibitors of ALK but less potent inhibitors of MET compared to PF-02341066. X-376 displayed potent antitumor activity in vivo with favorable pharmacokinetic and toxicity profiles.
Science. 2017 Dec 1;358(6367).
The target landscape of clinical kinase drugs
X-376 purchased from AbMole
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Source | Munich Industrial University (2018). Figure 36. X-376 (AbMole BioScience) |
| Method | Kinase binding of small molecule inhibitors | |
| Cell Lines | BT-474 cells, Caki-1 cells, KM-12 and HEK-293 cells | |
| Concentrations | 1 μM | |
| Incubation Time | 24 h | |
| Results | Notably, the photosensitizing effect of small molecule inhibitors can also be used for photodynamic therapy of cancer. |
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Source | Science (2017). Figure 4. X-376 (Abmole Bioscience) |
| Method | Cell viability and proliferation assays | |
| Cell Lines | A-431 and ACHN cells | |
| Concentrations | 50 nM | |
| Incubation Time | 72 h | |
| Results | Regardless of whether or not EGFR carried an activating mutation, the combination was always more effective in inhibiting cell viability and proliferation than any one drug alone. |
| Molecular Weight | 547.41 |
| Formula | C25H25Cl2FN6O3 |
| CAS Number | 1365267-27-1 |
| Solubility (25°C) | DMSO 90 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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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). |
| NVL-655
NVL-655 (ALK-IN-27) is a novel, brain-permeable, selective ALK inhibitor with antitumor activity. For Ba/F3 CLIP1-LTK cells, NVL-655 has an IC50 of 2.7 nM. NVL-655 (ALK-IN-27) can be used in studies related to ALK-positive non-small cell lung cancer (NSCLC). |
| APG-2449
APG-2449 is an orally active, potent ALK/ROS1/FAK inhibitor with anti-tumor activity in a mouse model of non-small cell lung cancer (NSCLC). |
| ALK2-IN-5
ALK2-IN-5, pyrazolopyrimidine compound, is an ALK2 inhibitor. |
| J-1048
J-1048 is an activin receptor-like kinase 5 (ALK5) inhibitor. |
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