中文名：羅比替尼（FGF401）

英文名：Roblitinib (FGF401)

純度：Moligand?，≥98%

貨號(hào)：R414051

Cas號(hào)：1708971-55-4

存儲(chǔ)溫度：-20°C儲(chǔ)存

運(yùn)輸條件：超低溫運(yùn)輸

產(chǎn)品介紹：

FGF401 is an inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon administration, FGF401 binds to and inhibits the activity of FGFR4, which leads to an inhibition of tumor cell proliferation in FGFR4-overexpressing cells. FGFR4 is a receptor tyrosine kinase upregulated in certain tumor cells and involved in tumor cell proliferation, differentiation, angiogenesis, and survival.

Information

Roblitinib (FGF401) Roblitinib (FGF401) is an FGFR4 -selective inhibitor with an IC50 of 1.1 nM. It binds in a reversible covalent manner to the FGFR4 kinase domain and shows at least 1,000 fold selectivity against of panel of 65 kinases in biochemical assays.

Targets

FGFR4 (Cell-free assay) 1.1 nM

In vitro

Roblitinib (FGF401) binds in a reversible covalent manner to the FGFR4 kinase domain and it inhibits FGFR4 with an IC50 of 1.1 nM. In biochemical assays, it shows at least 1,000 fold selectivity against of panel of 65 kinases and in a kinome wide scan, consisting of 456 kinases, FGFR4 was the only target of NVP-FGF401. FGF401 inhibits growth of HCC and gastric cancer cell lines expressing FG19, FGFR4 and βklotho.

In vivo

In xenograft animal models NVP-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. It has good oral PK properties and remarkable anti-tumor activity in mice bearing HCC tumor xenografts and PDX models that are positive for FGF19, FGFR4 and KLB.

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