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Roblitinib
- FGF 401 - NVP-FGF401
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C25H30N8O4
- MW: 506.56
Description
Roblitinib is a first-in-class, highly selective and potent FGFR4 inhibitor with an IC50 value of 1.1 nM. Roblitinib binds in a reversible covalent manner to the FGFR4 kinase domain. Developed for hepatocellular carcinoma and currently undergoing clinical evaluation for the treatment of FGFR4 and β-klotho positive solid tumors.
More Information
| Parent CAS No. | 1708971-55-4 |
|---|---|
| Chemical Name | N-(5-Cyano-4-(2-methoxyethylamino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide |
| SMILES | N1C2N(C(=O)NC3N=CC(C#N)=C(NCCOC)C=3)CCCC=2C=C(CN2CCN(C)CC2=O)C=1C=O |
| MFCD | N.A. |
| InChi | InChI=1S/C25H30N8O4/c1-31-7-8-32(23(35)15-31)14-18-10-17-4-3-6-33(24(17)29-21(18)16-34)25(36)30-22-11-20(27-5-9-37-2)19(12-26)13-28-22/h10-11,13,16H,3-9,14-15H2,1-2H3,(H2,27,28,30,36) |
| InChiKey | BHKDKKZMPODMIQ-UHFFFAOYSA-N |
| CID | 118036971 |
| Short Description | FGFR4 inhibitor |
References
- D Graus Porta et al. Abstract 2098: NVP-FGF401, a first-in-class highly selective and potent FGFR4 inhibitor for the treatment of HCC. Proceedings: AACR Annual Meeting 2017; April 1-5, 2017.
- T Knoepfel et al. 2-Formylpyridyl Ureas as Highly Selective Reversible-Covalent Inhibitors of Fibroblast Growth Factor Receptor 4. ACS Med Chem Lett. 2018 Feb 1;9(3):215-220.
- HS Schadt et al. Bile Acid Sequestration by Cholestyramine Mitigates FGFR4 Inhibition-Induced ALT Elevation. Toxicol Sci. 2018 May 1;163(1):265-278.
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