FGF-401 - CAS 1708971-55-4
Catalog number: B0084-007362
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C25H30N8O4
Molecular Weight:
506.56
COA:
Inquire
Targets:
FGFR
Description:
FGF-401 is an inhibitor of human fibroblast growth factor receptor 4 (FGFR4) (IC50= 1.9 nM) developed for the treatment of solid tumor.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-007362 10 mg $198 In stock
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Brife Description:
An inhibitor of FGFR4
Synonyms:
FGF401; FGF-401; FGF 401; roblitinib; 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
Solubility:
DMSO: 6 mg/mL (Need Ultrasonic)
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
Inquire
Boiling Point:
852.1±65.0 ℃ at 760 Torr
Density:
1.39±0.1 g/cm3
InChIKey:
BHKDKKZMPODMIQ-UHFFFAOYSA-N
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)
Canonical SMILES:
CN1CCN(C(=O)C1)CC2=C(N=C3C(=C2)CCCN3C(=O)NC4=NC=C(C(=C4)NCCOC)C#N)C=O
1.Bile Acid Sequestration by Cholestyramine Mitigates FGFR4 Inhibition-Induced ALT Elevation.
Schadt HS;Wolf A;Mahl JA;Wuersch K;Couttet P;Schwald M;Fischer A;Lienard M;Emotte C;Teng CH;Skuba E;Richardson TA;Manenti L;Weiss A;Graus Porta D;Fairhurst RA;Kullak-Ublick GA;Chibout SD;Pognan F;Kluwe W;Kinyamu-Akunda J Toxicol Sci. 2018 May 1;163(1):265-278. doi: 10.1093/toxsci/kfy031.
The FGF19- fibroblast growth factor receptor (FGFR4)-βKlotho (KLB) pathway plays an important role in the regulation of bile acid (BA) homeostasis. Aberrant activation of this pathway has been described in the development and progression of a subset of liver cancers including hepatocellular carcinoma, establishing FGFR4 as an attractive therapeutic target for such solid tumors. FGF401 is a highly selective FGFR4 kinase inhibitor being developed for hepatocellular carcinoma, currently in phase I/II clinical studies. In preclinical studies in mice and dogs, oral administration of FGF401 led to induction of Cyp7a1, elevation of its peripheral marker 7alpha-hydroxy-4-cholesten-3-one, increased BA pool size, decreased serum cholesterol and diarrhea in dogs. FGF401 was also associated with increases of serum aminotransferases, primarily alanine aminotransferase (ALT), in the absence of any observable adverse histopathological findings in the liver, or in any other organs. We hypothesized that the increase in ALT could be secondary to increased BAs and conducted an investigative study in dogs with FGF401 and coadministration of the BA sequestrant cholestyramine (CHO). CHO prevented and reversed FGF401-related increases in ALT in dogs in parallel to its ability to reduce BAs in the circulation.
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FGF-401 is an inhibitor of human fibroblast growth factor receptor 4 (FGFR4) (IC50= 1.9 nM) developed for the treatment of solid tumor.

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CAS 1708971-55-4 FGF-401

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