1355324-78-5Relevant articles and documents
Discovery of the first potent inhibitors of mutant IDH1 that lower tumor 2-HG in vivo
Popovici-Muller, Janeta,Saunders, Jeffrey O.,Salituro, Francesco G.,Travins, Jeremy M.,Yan, Shunqi,Zhao, Fang,Gross, Stefan,Dang, Lenny,Yen, Katharine E.,Yang, Hua,Straley, Kimberly S.,Jin, Shengfang,Kunii, Kaiko,Fantin, Valeria R.,Zhang, Shunan,Pan, Qiongqun,Shi, Derek,Biller, Scott A.,Su, Shinsan M.
supporting information, p. 850 - 855 (2013/01/15)
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.
