GRAU & PUREZAMoligand™?Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools.2mM in DMSO
Moligand™, 2mM in DMSO Moligand™ para fluxos de trabalho cromatográficos e analíticos sensíveis que exigem interferência mínima da linha de base.
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Armazenamento e envio
Store at -80°C Envio Dry ice packs + Cold packs. Consulte o COA específico do lote para obter as especificações exatas.
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Documentos de qualidade
SDS, COA, ficha técnica e folha de especificações disponíveis para download. COA específico do lote acessível por meio de pesquisa por número de lote.
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Comprovação documental
Citado em 0 publicações revisadas por pares nas áreas de cromatografia, síntese orgânica e reações de acoplamento cruzado.
Visão geral
Information
Roblitinib (FGF401) Roblitinib (FGF401) is an FGFR4 -selective inhibitor with an IC50 of 1.1 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 (Cell-free assay) 1.1 nM
In vitro
Roblitinib (FGF401) binds in a reversible covalent manner to the FGFR4 kinase domain and it inhibits FGFR4 with an IC50 of 1.1 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.
In vivo
In xenograft animal models NVP-FGF401 showed a consistent pharmacokinetic/pharmacodynamic (PK/PD) relationship with phospho-FGFR4 over total FGFR4 (p/tFGFR4) levels in tumor robustly inhibited in a dose dependent manner. It has good oral PK properties and remarkable anti-tumor activity in mice bearing HCC tumor xenografts and PDX models that are positive for FGF19, FGFR4 and KLB.
Roblitinib (FGF401) is an FGFR4-selective inhibitor with an IC50 of 1.1 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.
Condições de armazenamento de armazenamento
Store at -80°C
Enviado em
Dry ice packs + Cold packs
Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.
This compound belongs to the class of organic compounds known as naphthyridines. These are compounds containing a naphthyridine moiety, a naphthalene in which a carbon atom has been replaced by a nitrogen in each of the two rings. The naphthyridine skeleton can also be described as an assembly two fused pyridine rings, which do not share their nitrogen atom.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
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