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Association details:
Biomarker:IDH1 R132H
Cancer:Acute Myelogenous Leukemia
Drug:GSK321 (IDH1 inhibitor)
Direction:Sensitive
Evidence:
Evidence Level:
Sensitive: D – Preclinical
New
Title:

Novel IDH1 Mutant Inhibitors for Treatment of Acute Myeloid Leukemia

Excerpt:
...we treated IDH1 wild type (WT), R132G, R132C and R132H IDH1 mutant AML and bone marrow (BM) cells from healthy donors with 3 μM GSK321 or GSK990. Following 6 days of treatment in suspension culture, we observed a significant decrease in intracellular 2-HG with GSK321 (R132G, 0.13-fold ± 0.1-fold; R132C, 0.15-fold ± 0.2-fold; R132H, 0.29-fold), in contrast to cells treated with either DMSO or GSK990 (Fig. 3a).
DOI:
10.1038/nchembio.1930