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BAY-1436032 is an inhibitor of mutant isocitrate dehydrogenase 1 (IDH1; IC50 = 0.015 µM for both IDH1R132H and IDH1R132C).{65228} It is selective for mutant IDH1 over wild-type IDH1 and IDH2 (IC50s = 20 and >100 µM, respectively). BAY-1436032 inhibits production of ?-hydroxyglutaric acid (2-HG; Item Nos. 25894 | 16374) in HEK293 cells expressing IDH1R132H, IDH1R132C, IDH1R132G, IDH1R132S, and IDH1R132L, but not IDH1R100Q, IDH2R172K, IDH2R172W, or IDH2R172M. It also inhibits 2-HG production in LN-229 glioblastoma and HCT116 colorectal carcinoma cells overexpressing IDH1R132H (IC50s = 73 and 47 nM, respectively), as well as in HT-1080 sarcoma cells endogenously expressing IDH1R132C (IC50 = 135 nM). BAY-1436032 (150 mg/kg) reduces tumor growth and increases survival in an NCH551b IDH1R132H mutant secondary glioblastoma patient-derived xenograft (PDX) mouse model. It also induces myeloid differentiation of IDH1R132C mutant acute myeloid leukemia (AML) cells in mice when administered at doses of 45 and 150 mg/kg.{65229}
Territorial Availability: Available through Bertin Technologies only in France
| Size | 1 mg, 10 mg, 5 mg, 500 µg |
|---|---|
| Shipping | dry ice |
| CAS number | 1803274-65-8 |
| Molecular formula | C26H30F3N3O3 |
| Smiles | OC(CCC1=CC=C2N([C@@]3([H])CC(C)(C[C@H](C3)C)C)C(N([H])C4=CC=C(C=C4)OC(F)(F)F)=NC2=C1)=O |
| Molecular weight | 489,5 |
| Custom code | 2933.79 |
| 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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