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10.1021/ml300225h

http://scihub22266oqcxt.onion/10.1021/ml300225h
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C4025665!4025665!24900389
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suck abstract from ncbi


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pmid24900389      ACS+Med+Chem+Lett 2012 ; 3 (10): 850-5
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  • Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in Vivo #MMPMID24900389
  • Popovici-Muller J; Saunders J; Salituro FG; Travins JM; Yan S; Zhao F; Gross S; Dang L; Yen KE; Yang H; Straley KS; Jin S; Kunii K; Fantin VR; Zhang S; Pan Q; Shi D; Biller SA; Su SM
  • ACS Med Chem Lett 2012[Oct]; 3 (10): 850-5 PMID24900389show ga
  • Optimization of a series of R132H IDH1 inhibitors from a high throughput screen led to the first potent molecules that show robust tumor 2-HG inhibition in a xenograft model. Compound 35 shows good potency in the U87 R132H cell based assay and ?90% tumor 2-HG inhibition in the corresponding mouse xenograft model following BID dosing. The magnitude and duration of tumor 2-HG inhibition correlates with free plasma concentration.
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