Roblitinib | B3008

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 1.9 nM 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.

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 1.9 nM 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.

B3008 | Roblitinib DataSheet

Alternate Name/Synonyms: 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

Appearance: Pale-yellow Solid

Formulation:

CAS Number: 1708971-55-4

Structure Available?: TRUE

Peptide sequence:

Salt Form: FALSE

Molecular Formula: C₂₅H₃₀N₈O₄

Molecular Weight: 506.6

Cell-Permeable?: TRUE

Purity: >98%

Solubilities: ~5 mg/ml in DMSO (gently warm and vortex)

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: A potent inhibitor of FGFR4

MDL Number: MFCD31381923

PubChem CID: 118036971

SMILES: CN1CCN(C(=O)C1)CC2=C(N=C3C(=C2)CCCN3C(=O)NC4=NC=C(C(=C4)NCCOC)C#N)C=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