Territorial Availability: Available through Bertin Technologies only in France
- Synonyms
- 6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)-8-[3-[4-(1-oxo-2-propen-1-yl)-1-piperazinyl]propyl]-pyrido[2,3-d]pyrimidin-7(8H)-one
- Correlated keywords
- 1814961-21-1 PRN1371 panFGFR VEGFR 2 CSF 1R SNU16 RT 4
- Product Overview:
PRN-1371 is an irreversible covalent pan-FGFR inhibitor (IC50s = 0.7, 1.3, 4.4, and 19.3 nM for FGFR-1, -2, -3, and -4, respectively).{54899} It is selective for FGFR over VEGFR2 (IC50 = 705 nM) and a panel of 250 kinases (IC50s = >1 µM for all) but does inhibit colony stimulating factor 1 receptor (CSF1R) activity by greater than 90% at 1 µM. PRN-1371 inhibits proliferation in a panel of ten cancer cell lines containing various FGFR mutants (IC50s = 2-231 nM) and induces apoptosis in SNU-16 gastric and RT4 bladder cancer cells (EC50s = 15.9 and 11.8 nM, respectively). It reduces tumor growth in an SNU-16 mouse xenograft model and a patient-derived xenograft (PDX) mouse model of liver cancer when administered at a dose of 15 mg/kg twice per day.
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.