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Ensartinib

Cat. No. M28270
Ensartinib Structure
Synonym:

X-396

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Quality Control & Documentation
Biological Activity

Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.

Chemical Information
Molecular Weight 561.44
Formula C26H27Cl2FN6O3
CAS Number 1370651-20-9
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Yuxiang Ma, et al. J Thorac Dis. Ensartinib in advanced ALK-positive non-small cell lung cancer: a multicenter, open-label, two-staged, phase 1 trial

[2] Leora Horn, et al. JAMA Oncol. Ensartinib vs Crizotinib for Patients With Anaplastic Lymphoma Kinase-Positive Non-Small Cell Lung Cancer: A Randomized Clinical Trial

[3] Yunpeng Yang, et al. J Thorac Oncol. Decoding the Evolutionary Response to Ensartinib in Patients With ALK-Positive NSCLC by Dynamic Circulating Tumor DNA Sequencing

[4] Yang Wang, et al. Zhongguo Fei Ai Za Zhi. [Pharmacology and Clinical Evaluation of Ensartinib Hydrochloride Capsule]

[5] Yunpeng Yang, et al. Lancet Respir Med. Efficacy, safety, and biomarker analysis of ensartinib in crizotinib-resistant, ALK-positive non-small-cell lung cancer: a multicentre, phase 2 trial

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  Catalog
Abmole Inhibitor Catalog




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


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