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CAS No.: 1708971-55-4

Roblitinib Catalog No. CSN19757

Synonyms: FGF-401;NVP-FGF401;roblitinib

FGF401, an inhibitor of human fibroblast growth factor receptor 4 (FGFR4, IC50 = 1.1 nM), has potential antineoplastic activity.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述FGF401 is a first-in-class highly selective and potent FGFR4 inhibitor with IC50 value of 1.1nM. FGF401 showed a consistent pharmacokinetic/pharmacodynamic (PK/PD) relationship with phospho-FGFR4 over total FGFR4 (p/tFGFR4) levels in tumor robustly inhibited in a dose dependent manner in xenograft animal models. It exhibited anti-tumor activity across several xenograft animal models, as well as in patient-derived tumor xenografts (PDX) established in mice.
作用机制FGF401 binds in a reversible covalent manner to the FGFR4 kinase domain.^[1]
动物研究
剂量
Dog: 5 mg/kg - 45 mg/kg^[2] (p.o.)

给药途径
p.o.
临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT02325739 HCC Phase 1 Phase 2 Active, not recruiting July 15, 2020 -
参考文献

动物研究
剂量	Dog: 5 mg/kg - 45 mg/kg^[2] (p.o.)
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02325739	HCC	Phase 1 Phase 2	Active, not recruiting	July 15, 2020	-

[1] Abstract 2098: NVP-FGF401, a first-in-class highly selective and potent FGFR4 inhibitor for the treatment of HCC

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9741 mL
- 9.8705 mL
- 19.7410 mL
- 5 mM
- 0.3948 mL
- 1.9741 mL
- 3.9482 mL
- 10 mM
- 0.1974 mL
- 0.9870 mL
- 1.9741 mL

技术信息

CAS号

1708971-55-4

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H30N8O4

运输

蓝冰

分子量

506.56

别名

FGF-401;NVP-FGF401;roblitinib

溶解度

DMSO	5.0 mg/mL (9.9 mM)
Water	Insoluble
Ethanol	2.0 mg/mL (3.9 mM)

动物实验配方

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