| CAS NO: | 1370651-20-9 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| Molecular Weight (MW) | 561.44 |
|---|---|
| Formula | C26H27Cl2FN6O3 |
| CAS No. | 1370651-20-9 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 100 mg/mL (178.1 mM) |
| Water: <1 mg/mL | |
| Ethanol: 100 mg/mL (178.1 mM) | |
| SMILES Code | O=C(C1=NN=C(N)C(O[C@@H](C2=C(Cl)C=CC(F)=C2Cl)C)=C1)NC3=CC=C(C(N4CCN(C)CC4)=O)C=C3 |
| Synonyms | X396; X-396; X 396 |
| In Vitro | In vitro activity: Ensartinib is a novel, highly active 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 Ensartinib, albeit at higher concentrations required to block autophosphorylation of the wild-type fusion. Kinase Assay: Ensartinib (also known as X-396) is a novel, potent and specific ALK TKI with the IC50 less than 4 nM in Ambit assays. Cell Assay: 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. |
|---|---|
| In Vivo | Ensartinib demonstrates significant anti-tumor activity in vivo with favorable pharmacokinetic and safety profiles. Ensartinib shows high bioavailability and moderate half-lives in vivo. It significantly delays the growth of tumors compared to vehicle alone. Ensartinib could lead to higher efficacy against ALK-fusion positive brain metastases. It has demonstrated significant pre-clinical anti-tumor activity in both ALK TKI-naive and crizotinib-resistant models of ALK rearranged NSCLC. |
| Animal model | Nude mice |
| Formulation & Dosage | 0.5% HPMC, 0.4% Tween80, 99.1% DI water; 25mg/kg; oral |
| References | Cancer Res. 2011 Jul 15;71(14):4920-31. |
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