Ensartinib (X-396) is a potent and highly specific ALK small molecule tyrosine kinase inhibitors (TKIs). In Ambit kinome screens, cell growth inhibition studies, and surrogate kinase assays, Ensartinib (X-396) was more potent inhibitors of ALK but less potent inhibitors of MET compared to PF-02341066. Ensartinib (X-396) 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
Ensartinib purchased from AbMole
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Source | Munich Industrial University (2018). Figure 36. X-396 (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-396 (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 ≥ 22 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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| CPD-1224
CPD-1224 is an orally active derivative of ALK inhibitors to cereblon ligands. |
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Ack1 inhibitor 1 is a potent, selective, and orally active inhibitor of ACK1 kinase with an IC50 value of 2.1 nM. |
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Conteltinib (CT-707) is a potent second-generation mesenchymal lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) with antitumor activity for studies related to hepatocellular carcinoma (HCC). |
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