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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Choose Selective ALK Inhibitors
|Description||Ensartinib (X-396) is a novel, potent and specific ALK TKI with the IC50 less than 4 nM in Ambit assays.|
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. ALK autophosphorylation is significantly diminished by X-396, albeit at higher concentrations required to block autophosphorylation of the wild-type fusion.
|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.|
|In vitro||DMSO||100 mg/mL (178.11 mM)|
|Ethanol||100 mg/mL (178.11 mM)|
* 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.
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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|
|NCT03155620||Recruiting||Advanced Malignant Solid Neoplasm|Ann Arbor Stage III Childhood Non-Hodgkin Lymphoma|Ann Arbor Stage IV Childhood Non-Hodgkin Lymphoma|Childhood Langerhans Cell Histiocytosis|Histiocytic Sarcoma|Juvenile Xanthogranuloma|Malignant Glioma|Recurrent Central Nervous System Neoplasm|Recurrent Childhood Ependymoma|Recurrent Childhood Malignant Germ Cell Tumor|Recurrent Childhood Medulloblastoma|Recurrent Childhood Non-Hodgkin Lymphoma|Recurrent Childhood Rhabdomyosarcoma|Recurrent Childhood Soft Tissue Sarcoma|Recurrent Ewing Sarcoma|Recurrent Glioma|Recurrent Hepatoblastoma|Recurrent Langerhans Cell Histiocytosis|Recurrent Malignant Solid Neoplasm|Recurrent Neuroblastoma|Recurrent Osteosarcoma|Recurrent Peripheral Primitive Neuroectodermal Tumor|Refractory Central Nervous System Neoplasm|Refractory Childhood Malignant Germ Cell Tumor|Refractory Langerhans Cell Histiocytosis|Refractory Malignant Solid Neoplasm|Refractory Neuroblastoma|Rhabdoid Tumor|Stage III Osteosarcoma AJCC v7|Stage III Soft Tissue Sarcoma AJCC v7|Stage IV Osteosarcoma AJCC v7|Stage IV Soft Tissue Sarcoma AJCC v7|Stage IVA Osteosarcoma AJCC v7|Stage IVB Osteosarcoma AJCC v7|Wilms Tumor||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|
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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