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H3B-6527 is an inhibitor of FGF receptor 4 (FGFR4; IC50 = 50s = 320, 1,290, and 1,060 nM, respectively), as well as TAOK2, JNK2, and CSF1R (IC50s = 690, >10,000, and >10,000 nM, respectively). H3B-6527 increases the expression of the cytochrome P450 (CYP) isoform CYP7A1 and decreases phosphorylation of ERK1/2 in Hep3B hepatocellular carcinoma (HCC) cells in a concentration-dependent manner, indicating inhibition of the FGF19-FGFR4 signaling pathway. It also decreases cell growth (GI50 = 25 nM) and increases caspase-3/7 activity in Hep3B HCC cells. H3B-6527 selectively inhibits cell growth in HCC cell lines that express high levels of FGF19 and have high FGF19 protein levels. It reduces tumor growth in a Hep3B HCC mouse xenograft model, when administered at doses of 100 and 300 mg/kg, and in patient-derived xenograft models with high FGF19 expression. H3B-6527, in combination with PD 0332991 (palbociclib; Item No. 16273), induces tumor stasis in a JHH-7 mouse xenograft model.
Territorial Availability: Available through Bertin Technologies only in France
| Size | 1 mg, 10 mg, 25 mg, 5 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 1702259-66-2 |
| Molecular formula | C29H34Cl2N8O4 |
| Smiles | ClC1=C(NC(N(C2=CC(NC3=C(NC(C=C)=O)C=C(N4CCN(CC)CC4)C=C3)=NC=N2)C)=O)C(Cl)=C(OC)C=C1OC |
| Molecular weight | 629,5 |
| Custom code | 2933.59 |
| Formulation | A solid |
| Purity | ≥98% |
| UNSPSC code | 12352100 |
Cayman Chemical’s mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.
Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.
Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.
Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.
Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009
Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.
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