产品
编 号：F167739
分子式：C18H19F2N5O4
分子量：407.37
分子式：C18H19F2N5O4
分子量：407.37
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 1453208-66-6
产品详情
生物活性：
ASP5878 is an oral active inhibitor of FGFR 1, 2, 3, and 4, with IC50 values of 0.47 nM, 0.6 nM, 0.74 nM and 3.5 nM for FGFR 1, 2, 3, and 4 kinase activity. ASP5878 has potential antineoplastic activity.
体内研究：
ASP5878 (3 mg/kg，口服，每日一次) 在 Hep3B2.1-7 皮下异种移植和 HCC 原位异种移植小鼠模型中显示出抗肿瘤活性。 ASP5878 诱导 FGF19 收缩-表达 HCC 异种移植模型。Animal Model:Four-week-old male nude mice (CAnN.Cg-Foxn1nu/CrlCrlj [nu/nu]) (Hep3B2.1-7 cells inoculated subcutaneously).
Dosage:3 mg/kg.
Administration:Orally once daily from days 14 to 52.
Result:Induced tumor regression by 9% and 88% at 1 and 3 mg/kg, respectively, without affecting the body weight for 14 days.Induced the suppression of FGFR4 phosphorylation, mobility shift of FRS2, and suppression of ERK phosphorylation.
Animal Model:HCC orthotopic xenograft model (mouse).
Dosage:3 mg/kg.
Administration:Orally once daily for 24 days.
Result:Exhibited a lower tumor burden than vehicle- and sorafenibtreated mice.Induced sustained tumor regression without tumor regrowth.
体外研究：
ASP5878 在大多数人类 HCC 细胞系中显示出有效的抗增殖活性。 ASP5878 以浓度依赖性方式抑制 FGFR4 磷酸化。ASP5878 处理导致磷酸化抑制、FRS2 迁移率变化和 ERK 磷酸化抑制。
ASP5878 is an oral active inhibitor of FGFR 1, 2, 3, and 4, with IC50 values of 0.47 nM, 0.6 nM, 0.74 nM and 3.5 nM for FGFR 1, 2, 3, and 4 kinase activity. ASP5878 has potential antineoplastic activity.
体内研究：
ASP5878 (3 mg/kg，口服，每日一次) 在 Hep3B2.1-7 皮下异种移植和 HCC 原位异种移植小鼠模型中显示出抗肿瘤活性。 ASP5878 诱导 FGF19 收缩-表达 HCC 异种移植模型。Animal Model:Four-week-old male nude mice (CAnN.Cg-Foxn1nu/CrlCrlj [nu/nu]) (Hep3B2.1-7 cells inoculated subcutaneously).
Dosage:3 mg/kg.
Administration:Orally once daily from days 14 to 52.
Result:Induced tumor regression by 9% and 88% at 1 and 3 mg/kg, respectively, without affecting the body weight for 14 days.Induced the suppression of FGFR4 phosphorylation, mobility shift of FRS2, and suppression of ERK phosphorylation.
Animal Model:HCC orthotopic xenograft model (mouse).
Dosage:3 mg/kg.
Administration:Orally once daily for 24 days.
Result:Exhibited a lower tumor burden than vehicle- and sorafenibtreated mice.Induced sustained tumor regression without tumor regrowth.
体外研究：
ASP5878 在大多数人类 HCC 细胞系中显示出有效的抗增殖活性。 ASP5878 以浓度依赖性方式抑制 FGFR4 磷酸化。ASP5878 处理导致磷酸化抑制、FRS2 迁移率变化和 ERK 磷酸化抑制。
产品资料
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