[CAS NO. 1708971-55-4] Roblitinib (FGF401)
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PRODUCTS SPECIFICATIONS [1708971-55-4]
Store
Catalog
SLK-S8548
Brand
Selleck
CAS
1708971-55-4
DESCRIPTION [1708971-55-4]
Overview
| MDL | MFCD31381923 |
|---|---|
| Molecular Weight | 506.56 |
| Molecular Formula | C25H30N8O4 |
| SMILES | O=C(N1CCCC2=C1N=C(C=O)C(CN3C(CN(C)CC3)=O)=C2)NC4=NC=C(C#N)C(NCCOC)=C4 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 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 |
| 50 mM | - | - | - |
Description
Roblitinib (FGF401) is an -selective inhibitor with an IC50 of 1.9 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 [1] (Cell-free assay) |
| 1.9 nM |
In vitro
Roblitinib (FGF401) binds in a reversible covalent manner to the FGFR4 kinase domain and it inhibits FGFR4 with an IC50 of 1.9 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.
References
[1] Diana Graus Porta, et al. AACR Cancer Res. 2017, 77(13 Suppl):Abstract nr 2098.
[2] Hierro C, et al. Semin Oncol. 2015, 42(6):801-19.
[3] Andreas Weiss, et al. AACR Cancer Res. 2017, 77(13 Suppl):Abstract nr 2103.
[4]Nicole B, et al. Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors.WO2015059668A1.
[2] Hierro C, et al. Semin Oncol. 2015, 42(6):801-19.
[3] Andreas Weiss, et al. AACR Cancer Res. 2017, 77(13 Suppl):Abstract nr 2103.
[4]Nicole B, et al. Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors.WO2015059668A1.
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