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Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in Vivo.

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Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in Vivo.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	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.
Description	Country affiliation: United States Author Affiliation: Popovici-Muller J ( Agios Pharmaceuticals , 38 Sidney Street, Cambridge, Massachusetts 02139, United States.); Saunders JO ( Ember Therapeutics , 855 Boylston Street, 11th Floor, Suite B, Boston, Massachusetts 02116, United States.); Salituro FG ( Sage Therapeutics , 215 First Street, Cambridge, Massachusetts 02141, United States.); Travins JM ( Agios Pharmaceuticals , 38 Sidney Street, Cambridge, Massachusetts 02139, United States.); Yan S ( Schrödinger, Inc. , 120 West 45th Street, New York, New York 10036, United States.); Zhao F ( Sundia MediTech Company, Ltd. , Building 8, 388 Jialilue Road, Zhangjiang High-Tech Park, Shanghai 201203, China.); Gross S ( Agios Pharmaceuticals , 38 Sidney Street, Cambridge, Massachusetts 02139, United States.); Dang L ( Agios Pharmaceuticals , 38 Sidney Street, Cambridge, Massachusetts 02139, United States.); Yen KE ( Agios Pharmaceuticals , 38 Sidney Street, Cambridge, Massachusetts 02139, United States.); Yang H ( Agios Pharmaceuticals , 38 Sidney Street, Cambridge, Massachusetts 02139, United States.); Straley KS ( Agios Pharmaceuticals , 38 Sidney Street, Cambridge, Massachusetts 02139, United States.); Jin S ( Agios Pharmaceuticals , 38 Sidney Street, Cambridge, Massachusetts 02139, United States.); Kunii K ( Agios Pharmaceuticals , 38 Sidney Street, Cambridge, Massachusetts 02139, United States.); Fantin VR ( Oncology Research Unit, Pfizer Worldwide Research and Development , La Jolla Laboratories, San Diego, California 92121, United States.); Zhang S ( Shanghai ChemPartner Co., LTD , 998 Halei Road, Zhangjiang Hi-tech Park, Pudong New Area, Shanghai 201203, China.); Pan Q ( Shanghai ChemPartner Co., LTD , 998 Halei Road, Zhangjiang Hi-tech Park, Pudong New Area, Shanghai 201203, China.); Shi D ( Shanghai ChemPartner Co., LTD , 998 Halei Road, Zhangjiang Hi-tech Park, Pudong New Area, Shanghai 201203, China.); Biller SA ( Agios Pharmaceuticals , 38 Sidney Street, Cambridge, Massachusetts 02139, United States.); Su SM ( Agios Pharmaceuticals , 38 Sidney Street, Cambridge, Massachusetts 02139, United States.)
Abstract	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 â¼90% 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.
File Format	HTM / HTML
e-ISSN	19485875
DOI	10.1021/ml300225h
Journal	ACS Medicinal Chemistry Letters
Issue Number	10
Volume Number	3
Language	English
Publisher	American Chemical Society
Publisher Date	2012-10-11
Publisher Place	United States
Access Restriction	Open
Subject Keyword	Discipline Chemistry
Content Type	Text
Resource Type	Article

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Discovery of the FirstPotent Inhibitors of MutantIDH1 That Lower Tumor 2-HG in Vivo

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