BAY-1436032产品描述：BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.IC50 & Target: IDH1^[1]In Vitro: BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor. BAY-1436032 inhibits intracellular (R)-2-hydroxyglutarate (R-2HG) production in mouse hematopoietic cells expressing IDH1R132H or IDH1R132C with IC₅₀s of 60 and 45?nM, respectively. R-2HG levels are not reduced in IDH2R140Q and IDH2R172K expressing mouse hematopoietic cells by BAY-1436032 at concentrations up to 10?μM. Colony growth is inhibited by 50% at a concentration of 0.1?μM BAY-1436032, while concentrations up to 100?μM do not suppress colony growth of patient-derived IDH1 wild-type AML cells. On morphologic evaluation myelomonocytic differentiation of myeloid progenitors is strongly induced by BAY-1436032^[1].In Vivo: Long-term exposure to once daily oral BAY-1436032 reveals nearly complete suppression of (R)-2-hydroxyglutarate (R-2HG) production with 150?mg/kg BAY1436032. White blood cell counts constantly increase in vehicle-treated mice and, at a lower rate, in animals receiving 45?mg/kg BAY-1436032, while they remain constant in the 150?mg/kg cohort. Hemoglobin levels are slightly lower in the vehicle and 45?mg/kg groups as compare to the 150?mg/kg cohort at day 60, while platelet counts are significantly reduced in vehicle and 45?mg/kg BAY-1436032 treated mice compare to the 150?mg/kg cohort at day 60. All mice receiving 150?mg/kg BAY-1436032 survive with minimal hCD45⁺ cell load in their peripheral blood until the end of observation at day 150 after treatment start (P<0.001), while vehicle-treated animals die from leukemia with a median survival of 91 days. Mice treated with 45?mg/kg BAY-1436032 display intermediate levels of CD14/CD15 expression^[1].
产品链接：www.medchemexpress.com/BAY-1436032.html

研究领域：Metabolic Enzyme/Protease

靶点：Isocitrate Dehydrogenase (IDH)

相关产品：Enasidenib  |  Ivosidenib  |  AGI-5198  |  AGI-6780  |  Mutant IDH1 inhibitor  |  GSK864  |  Mutant IDH1-IN-1  |  Mutant IDH1-IN-2  |  Vorasidenib  |  IDH-305  |  



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更新时间：2024/1/2 10:10:55