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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Biological Activity

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

Protocol

Cell Research:

[1]

+ Expand
  • 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:

[1]

+ Expand
  • 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
Formula

C26H27Cl2FN6O3

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
NCT03536481 Not yet recruiting Lung Cancer Betta Pharmaceuticals Co.Ltd. May 31 2018 Phase 1
NCT03215693 Recruiting Non-Small Cell Lung Cancer Betta Pharmaceuticals Co.Ltd. September 28 2017 Phase 2
NCT03213652 Recruiting Advanced Malignant Solid Neoplasm|ALK Fusion Protein Expression|ALK Gene Mutation|ALK Gene Translocation|Ann Arbor Stage III Childhood Non-Hodgkin Lymphoma|Ann Arbor Stage IV Childhood Non-Hodgkin Lymphoma|Histiocytosis|Recurrent Childhood Central Nervous System Neoplasm|Recurrent Childhood Non-Hodgkin Lymphoma|Recurrent Malignant Solid Neoplasm|Recurrent Neuroblastoma|Refractory Central Nervous System Neoplasm|Refractory Malignant Solid Neoplasm|Refractory Neuroblastoma|Refractory Non-Hodgkin Lymphoma|ROS1 Fusion Positive|ROS1 Gene Mutation|ROS1 Gene Translocation National Cancer Institute (NCI) July 24 2017 Phase 2
NCT02959619 Recruiting Solid Tumor|Non-Small Cell Lung Cancer Metastatic Betta Pharmaceuticals Co.Ltd. November 2016 Phase 1
NCT02767804 Recruiting Non-small Cell Lung Cancer Xcovery Holding Company LLC June 2016 Phase 3
NCT01625234 Recruiting Advanced Solid Tumors|Non-small Cell Lung Cancer Xcovery Holding Company LLC June 2012 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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ALK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID