MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Ensartinib hydrochloride

CAS No. : 2137030-98-7

MCE 站：Ensartinib hydrochloride

产品活性：Ensartinib hydrochloride (X-396 hydrochloride) 是一种有效的双重的 ALK/MET 抑制剂，IC₅₀ 分别 <0.4 nM 和 0.74 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：ALK  |  c-Met/HGFR

In Vitro: Ensartinib (X-396) is a potent ａnd dual ALK/MET inhibitor with IC₅₀s of <0.4 nM ａnd 0.74 nM, respectively. Ensartinib is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC₅₀: 15 nM). Ensartinib is also potent in H2228 lung cancer cells harboring EML4-ALK E6a/b; A20 (IC₅₀: 45 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring NPM-ALK (IC₅₀: 9 nM).

In Vivo: Ensartinib (X-396) shows substantial bioavailability ａnd moderate half-lives in vivo. Nude mice harboring H3122 xenografts are treated with Ensartinib at 25 mg/kg bid. Ensartinib significantly delays the growth of tumors compared to vehicle alone. In the xenograft experiments, Ensartinib appears well-tolerated in vivo. Mouse weight is unaffected by Ensartinib treatment. Drug-treated mice appear healthy ａnd do not display any signs of compound related toxicity. To further assess potential side effects of Ensartinib, additional systemic toxicity ａnd toxico-kinetic studies are performed in Sprague Dawley (SD) rats. Following 10 days of repeated oral administration of Ensartinib at 20, 40, 80 mg/kg in SD rats, all animals survive to study termination. The no significant toxicity (NST) levels are determined to be 80 mg/kg for Ensartinib. At NST levels, Ensartinib achieves an AUC of 66 μM×hr ａnd a C_max of 7.19 μM.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Anti-COVID-19 Compound Library  |  Orally Active Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  A 83-01  |  PHA-665752  |  2-Phospho-L-ascorbic acid trisodium  |  AZD-3463  |  SU11274  |  SRI 31215 TFA  |  ALK inhibitor 1  |  c-Met inhibitor 1  |  X-376  |  HG-14-10-04  |  Tyrosine kinase inhibitor  |  6-Demethoxytangeretin  |  ALK inhibitor 2  |  JH-VIII-157-02  |  ALK/ROS1-IN-1  |  c-met-IN-1  |  F-1  |  Meleagrin  |  Norleual  |  TGFβRI-IN-2  |  TL13-110  |  TL13-22  |  Ensartinib  |  WY-135

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。