Ensartinib

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.

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 K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information

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.
	Rating

	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.
	Rating

Product Citations

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  Science. 2017 Dec 1;358(6367).

  The target landscape of clinical kinase drugs
  Ensartinib purchased from AbMole

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.