Catalog No.: PC-35173Not For Human Use, Lab Use Only.
IDH889 (IDH-889) is a potent, selective, brain penetrant, orally active IDH1 R132H mutant with IC50 of 20 nM, with good overall selectivity vs the wt IDH1.
IDH889 (IDH-889) is a potent, selective, brain penetrant, orally active IDH1 R132H mutant with IC50 of 20 nM, with good overall selectivity vs the wt IDH.
IDH889 binds into an allosteric, induced-fit pocket in IDH1R132H, shows potent cellular inhibition of 2-HG production in the engineered HCT116-IDH1R132H cell line with IC50 of 14 nM.
IDH889 inhibits 2-HG inhibition, modulates mutant IDH1-dependent DNA methylation changes in vivo.
IDH889 causes time-dependent changes, preferential hypomethylation of the loci in mutant cells.
IDH889 shows robust reduction of tumor derived 2-HG in a murine IDH1 mutant tumor xenograft model.
In addition to the potential treatment of AML, chondrosarcoma, cholangiocarcinoma, and other forms of mutant-IDH1 driven cancers, IDH889 demonstrates brain penetrant exposure.
