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Chemical Structure : Ensartinib dihydrochloride
CAS No.: 2137030-98-7
Catalog No.: PC-21789Not For Human Use, Lab Use Only.
Ensartinib (X-396) dihydrochloride 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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|---|---|---|---|
| 5 mg | $148 | In stock | |
| 10 mg | $228 | In stock | |
| 25 mg | $368 | In stock | |
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| 100 mg | Get quote |
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Ensartinib (X-396) dihydrochloride 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.
| M.Wt | 634.36 | |
| Formula | C26H29Cl4FN6O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
6-amino-5-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-N-(4-((3R,5S)-3,5-dimethylpiperazine-1-carbonyl)phenyl)pyridazine-3-carboxamide dihydrochloride |
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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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