BAY-1436032 是一种新型的泛突变异柠檬酸脱氢酶 1 (IDH1) 抑制剂。

BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.

Solid

IDH1

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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/k

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[1]. Chaturvedi A, et al. Pan-mutant-IDH1 inhibitor BAY1436032 is highly effective against human IDH1 mutant acute myeloid leukemia in vivo. Leukemia. 2017 Oct;31(10):2020-2028.

In Vitro: DMSO : 125 mg/mL (255.35 mM; Need ultrasonic and warming)配制储备液