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
|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|
|Incubation Time||24 h|
|Results||Notably, the photosensitizing effect of small molecule inhibitors can also be used for photodynamic therapy of cancer.|
|Source||Science (2017). Figure 4. X-396 (Abmole Bioscience)|
|Method||Cell viability and proliferation assays|
|Cell Lines||A-431 and ACHN cells|
|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.|
|Solubility (25°C)||DMSO ≥ 22 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Related ALK Products|
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J-1048 is an activin receptor-like kinase 5 (ALK5) inhibitor.
CPD-1224 is an orally active derivative of ALK inhibitors to cereblon ligands.
|Ack1 inhibitor 1
Ack1 inhibitor 1 is a potent, selective, and orally active inhibitor of ACK1 kinase with an IC50 value of 2.1 nM.
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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