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Ensartinib

Chemical Structure : Ensartinib

CAS No.: 1370651-20-9

Ensartinib (X396, X-396)

Catalog No.: PC-21788Not For Human Use, Lab Use Only.

Ensartinib (X-396) is a potent, selective and second-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) with biochemical IC50 of <0.4 nM, inhibits MET with IC50 of 0.74 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Ensartinib (X-396) is a potent, selective and second-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) with biochemical IC50 of <0.4 nM, inhibits MET with IC50 of 0.74 nM.
Ensartinib (X-396) is more potent ALK inhibitors than PF-02341066 (PF-1066).
Ensartinib (X-396) potently inhibits H3122 lung cancer cells harboring EML4-ALK E13;A20 (variant 1) with IC50 of 15 nM, 10-fold more potent than PF-02341066.
Ensartinib (X-396) display less activity against MET than PF-1066.
Ensartinib (X-396) (25mg/kg bid) inhibits tumore growth against H3122 xenografts.
Ensartinib (X-396) is effective against multiple ALK variants found in NSCLC, including ALK mutations associated with acquired resistance to PF-1066.
Ensartinib (X-396) is synergistic with mTOR inhibitor rapamycin against ALK fusion positive lung cancer cell lines.

Physicochemical Properties

M.Wt 561.44
Formula C26H27Cl2FN6O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-{4-[(3R,5S)-3,5-dimethylpiperazine-1-carbonyl]phenyl}pyridazine-3-carboxamide

References

1. Horn L, et al. Clin Cancer Res. 2018 Jun 15;24(12):2771-2779.

2. Christine M Lovly, et al. Cancer Res. 2011 Jul 15;71(14):4920-31.

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