Ensartinib (X-396)

Catalog No.S8230

Ensartinib (X-396) Chemical Structure

Molecular Weight(MW): 561.44

Ensartinib (X-396) is a novel, potent and specific ALK TKI with the IC50 less than 4 nM in Ambit assays.

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Description Ensartinib (X-396) is a novel, potent and specific ALK TKI with the IC50 less than 4 nM in Ambit assays.
Met [1]
(Ambit assay)
ALK [1]
(Ambit assay)
0.74 nM <4 nM
In vitro

Ensartinib is a novel, potent anaplastic lymphoma kinase (ALK) small molecule tyrosine kinase inhibitor (TKI) with additional activity against MET, ABL, Axl, EPHA2, LTK, ROS1 and SLK[2]. ALK autophosphorylation is significantly diminished by X-396, albeit at higher concentrations required to block autophosphorylation of the wild-type fusion[1].

In vivo X-396 displays potent anti-tumor activity in vivo with favorable pharmacokinetic and toxicity profiles. X-396 shows substantial bioavailability and moderate half-lives in vivo. It significantly delays the growth of tumors compared to vehicle alone. X-396 could lead to higher efficacy against ALK-fusion positive brain metastases. It has demonstrated significant pre-clinical anti-tumor activity in both ALK TKI-naïve and crizotinib-resistant models of ALK rearranged NSCLC[1].


Cell Research:


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  • Cell lines: H3122 and H2228 lung cancer cells, SUDHL-1 lymphoma cells, SY5Y neuroblastoma cells
  • Concentrations: 10, 100, 1000 nM
  • Incubation Time: 72 h
  • Method:

    H3122 lung cancer cells containing the EML4-ALK E13;A20 fusion, H2228 lung cancer cells harboring the EML4-ALK E6a/b;A20 fusion, SUDHL-1 lymphoma cells containing NPM-ALK fusion, and SY5Y neuroblastoma cells with an activating mutation within the ALK kinase domain (ALK F1174L) are treated with ALK TKIs or vehicle for 72h. Cell titer blue assays are performed to assess growth inhibition.

    (Only for Reference)
Animal Research:


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  • Animal Models: Nude mice
  • Formulation: 0.5% HPMC, 0.4% Tween80, 99.1% DI water
  • Dosages: 25mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (178.11 mM)
Ethanol 100 mg/mL (178.11 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 561.44


CAS No. 1370651-20-9
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03737994 Not yet recruiting ALK Gene Rearrangement|ALK Positive|Non-Squamous Non-Small Cell Lung Carcinoma|Stage IV Lung Cancer AJCC v8|Stage IVA Lung Cancer AJCC v8|Stage IVB Lung Cancer AJCC v8 National Cancer Institute (NCI) January 13 2019 Phase 2
NCT03574402 Not yet recruiting Carcinoma Non-Small-Cell Lung Guangdong Association of Clinical Trials July 1 2018 Phase 2
NCT03608007 Recruiting Lung Cancer|ROS1 Gene Rearrangement Betta Pharmaceuticals Co.Ltd. June 15 2018 Phase 2
NCT03536481 Not yet recruiting Lung Cancer Betta Pharmaceuticals Co.Ltd. May 31 2018 Phase 1
NCT03510611 Enrolling by invitation Non-Small Cell Lung Cancer Betta Pharmaceuticals Co.Ltd. March 19 2018 Phase 1
NCT03420508 Recruiting Melanoma Memorial Sloan Kettering Cancer Center|Xcovery Holding Company LLC January 10 2018 Phase 2

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ALK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID