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X-376

產品活性：X-376 是一種有效的高特異性 ALK 酪氨酸激酶抑制劑 (TKI) (IC₅₀=0.61 nM)。X-376 是 MET 的較低效抑制劑 (IC₅₀=0.69 nM)。X-376 具有有效的抗腫瘤活性。

研究領域：Protein Tyrosine Kinase/RTK

作用靶點：Anaplastic lymphoma kinase (ALK)  |  c-Met/HGFR

In Vitro: The ability of X-376 to inhibit the growth of different cancer cell lines harboring ALK fusions or point mutations is tested. X-376 is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC₅₀: 77 nM). X-376 is also potent in H2228 lung cancer cells harboring EML4-ALK E6a/b; A20 (IC₅₀: 57 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring NPM-ALK (IC₅₀: 32 nM). X-376 also inhibits SY5Y neuroblastoma cells harboring ALK F1174L, MKN-45 gastric carcinoma cells harboring MET dependent, HepG2 cells and PC-9 lung cancer cell lines harboring EGFR exon 19 del with IC₅₀s of 142 nM, 150 nM, 15.137 μM and 3.062 μM, respectively.

In Vivo: The effects of X-376 in vivo against H3122 xenografts are examined. A pharmacokinetic study reveals that X-376 shows substantial bioavailability and moderate half-lives in vivo. Nude mice harboring H3122 xenografts are treated with X-376 at 50 mg/kg bid. X-376 significantly delays the growth of tumors compared to vehicle alone. In the xenograft experiments, X-376 appears well-tolerated in vivo. Mouse weight is unaffected by X-376 treatment. Drug-treated mice appear healthy and do not display any signs of compound related toxicity. To further assess potential side effects of X-376, additional systemic toxicity and toxico-kinetic studies are performed in Sprague Dawley (SD) rats. Following 10 days of repeated oral administration of X-376 at 25, 50, 100 mg/kg in SD rats, all animals survive to study termination. The no significant toxicity (NST) levels are determined to be 50 mg/kg for X-376. At NST levels, X-376 achieves an AUC of 41 μM×hr and a C_max of 5.04 μM.

相關產品：Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Angiogenesis-Related Compound Library  |  Anti-Liver Cancer Compound Library   |  Anti-Colorectal Cancer Compound Library   |  Cancer Stem Cells Compound Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  AMG-208  |  DS-1205b free base  |  ALK/ROS1-IN-1  |  c-Met-IN-1  |  Ceritinib  |  Glumetinib  |  KRCA-0008  |  Savolitinib  |  Iruplinalkib  |  c-Met-IN-11  |  ABN401  |  Foretinib  |  ALK-IN-22  |  JH-VIII-157-02  |  Bafisontamab  |  MK-2461  |  Dalmelitinib  |  MK-8033 hydrochloride  |  NVP-TAE 684  |  c-Met-IN-12  |  MET kinase-IN-4  |  Cabozantinib  |  TL13-110  |  Brigatinib-¹³C₆  |  Alectinib  |  Zotizalkib  |  M4K2234  |  Con B-1  |  Ficonalkib

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