型号:
产品价格:电议      采购度:1369      原产地:美洲
发布时间:2022/1/22 1:46:09 所属地区:国外 国外
简要描述:
Zoligratinib (Debio 1347) 是口服可用,选择性的 FGFR 抑制剂,抑制FGFR1,FGFR2和 FGFR3的IC50 ,,22 and 290 nM。
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CAS No. : 1265229-25-1
MCE 站:Zoligratinib
产品活性:Zoligratinib (Debio 1347) 是口服可用,选择性的 FGFR 抑制剂,抑制FGFR1,FGFR2和 FGFR3的IC50 值分别为9.3,7.6,22 and 290 nM。
研究领域:Protein Tyrosine Kinase/RTK
作用靶点:FGFR
In Vitro: Zoligratinib is well balanced in cellular antiproliferative activity against SNU-16 and stability in human liver microsome. The selectivity of 8 to inhibit FGFR over KDR is suggested to be caused by the difference in the interaction with M535 in FGFR1 and L889 in KDR. The IC50 of Zoligratinib is 29 nM for FGF-dependent proliferation and 780 nM for VEGF-dependent proliferation.
In Vivo: Zoligratinib treatment shows a dose-dependent tumor regression (tumor growth inhibition (TGI)=106% at 30 mg/kg and 147% at 100 mg/kg) without apparent body weight loss. Zoligratinib treatment also shows significant in vivo efficacy in xenograft mice models with FGFR genetic alterations, such as KG1 (leukemia, FGFR1OP-FGFR1 fusion), MFE280 (endometrial cancer, FGFR2 S252W mutation), UM-UC-14 (bladder cancer, FGFR3 S249C mutation), and RT112/84 (bladder cancer, FGFR3-TACC3 fusion).
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更新时间:2024/1/2 10:20:04
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