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Ensartinib

Cat. No. M1743
Ensartinib Structure
Synonym:

X-396

Size Price Availability Quantity
2mg USD 120 In stock
5mg USD 290 In stock
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Quality Control
Biological Activity

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,X-396 was more potent inhibitors of ALK but less potent inhibitors of MET compared to PF-02341066. X-396 displayed potent antitumor activity in vivo with favorable pharmacokinetic and toxicity profiles.

Product Citations
Customer Product Validations & Biological Datas
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.
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 547.41
Formula C25H25Cl2FN6O3
CAS Number 1365267-27-1
Purity >99%
Solubility DMSO
Storage at -20°C
References

Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinase inhibitors.
Lovly CM et al. Cancer Res. 2011 Jul 15;71(14):4920-31. PMID: 21613408.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Ensartinib, X-396 supplier, ALK, inhibitors

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