Roblitinib Biochemical

Roblitinib

Cat. Num. AAA8400449

• Purity: >98%
• Synonyms: Roblitinib; FGF401; N-[5-cyano-4-(2-methoxyethylamino)pyridin-2-yl]-7-formyl-6-[(4-methyl-2-oxopiperazin-1-yl)methyl]-3; 4-dihydro-2H-1; 8-naphthyridine-1-carboxamide; N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3; 4-dihydro-1; 8-naphthyridine-1(2H)-carboxamide; Roblitinib biochemical

• Specificity: A potent inhibitor of FGFR4
• Purity/Purification: >98%
• Form/Format: Pale-yellow Solid

• Solubilities: ~5mg/ml in DMSO (gently warm and vortex)
• Molecular Formula: C??H??N?O?
• 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)
• InChi Key: BHKDKKZMPODMIQ-UHFFFAOYSA-N
• SMILES: CN1CCN(C(=O)C1)CC2=C(N=C3C(=C2)CCCN3C(=O)NC4=NC=C(C(=C4)NCCOC)C#N)C=O
• CAS Number: 1708971-55-4
• MDL Number: MFCD31381923
• PubChem CID: 118036971
• Preparation and Storage: Store at -20 degree C; Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.; Shelf Life: Est.~36 months; Country of Origin: USA

Structure

Related Product Information for Roblitinib biochemical

Roblitinib is a reversible-covalent inhibitor of fibroblast growth factor receptor 4 (FGFR4) tyrosine kinase. It shows 1000-fold selectivity for FGFR4 over FGFR1/2/3 and other kinases, with an IC50 value of 1.9nM against FGFR4. It shows potent antitumor activity in mice bearing Hepatocellular carcinoma (HCC) tumor xenografts and patient-derived tumor xenograft PDX models. FGF401 has entered phase I/II clinical trials to evaluate its safety and efficacy in HCC and other solid tumors. It leads to upregulation of bile acid synthesis and a subsequent increase in ALT expression in preclinical studies, which can be prevented by combination with the bile acid sequestrant cholestyramine.

Product Categories/Family for Roblitinib biochemical

Web Categories; Enzyme Inhibitors; Protein Kinase Inhibitors; Protein Kinase Inhibitors (A-Z); Enzyme Inhibitors (A-Z); Biochemicals; Biochemicals (A-Z); Other Protein Kinase Inhibitors

References

https://pubchem.ncbi.nlm.nih.gov/compound/118036971