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Discovery of 6-[(3S,4S)-4-Amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methyl-3,4-dihydropyrimidin-4-one (IACS-15414), a Potent and Orally Bioavailable SHP2 Inhibitor.
Czako, Barbara; Sun, Yuting; McAfoos, Timothy; Cross, Jason B; Leonard, Paul G; Burke, Jason P; Carroll, Christopher L; Feng, Ningping; Harris, Angela L; Jiang, Yongying; Kang, Zhijun; Kovacs, Jeffrey J; Mandal, Pijus; Meyers, Brooke A; Mseeh, Faika; Parker, Connor A; Yu, Simon S; Williams, Christopher C; Wu, Qi; Di Francesco, Maria Emilia; Draetta, Giulio; Heffernan, Timothy; Marszalek, Joseph R; Kohl, Nancy E; Jones, Philip.
Affiliation
  • Czako B; IACS (Institute for Applied Cancer Science), University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Sun Y; TRACTION (Translational Research to AdvanCe Therapeutics and Innovation in Oncology) University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • McAfoos T; IACS (Institute for Applied Cancer Science), University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Cross JB; IACS (Institute for Applied Cancer Science), University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Leonard PG; IACS (Institute for Applied Cancer Science), University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Burke JP; IACS (Institute for Applied Cancer Science), University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Carroll CL; IACS (Institute for Applied Cancer Science), University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Feng N; TRACTION (Translational Research to AdvanCe Therapeutics and Innovation in Oncology) University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Harris AL; TRACTION (Translational Research to AdvanCe Therapeutics and Innovation in Oncology) University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Jiang Y; IACS (Institute for Applied Cancer Science), University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Kang Z; IACS (Institute for Applied Cancer Science), University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Kovacs JJ; TRACTION (Translational Research to AdvanCe Therapeutics and Innovation in Oncology) University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Mandal P; IACS (Institute for Applied Cancer Science), University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Meyers BA; TRACTION (Translational Research to AdvanCe Therapeutics and Innovation in Oncology) University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Mseeh F; IACS (Institute for Applied Cancer Science), University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Parker CA; IACS (Institute for Applied Cancer Science), University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Yu SS; IACS (Institute for Applied Cancer Science), University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Williams CC; IACS (Institute for Applied Cancer Science), University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Wu Q; IACS (Institute for Applied Cancer Science), University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Di Francesco ME; IACS (Institute for Applied Cancer Science), University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Draetta G; Department of Genomic Medicine, The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, United States.
  • Heffernan T; TRACTION (Translational Research to AdvanCe Therapeutics and Innovation in Oncology) University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Marszalek JR; TRACTION (Translational Research to AdvanCe Therapeutics and Innovation in Oncology) University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
  • Kohl NE; Navire Inc., 421 Kipling Street, Palo Alto, California 94301, United States.
  • Jones P; IACS (Institute for Applied Cancer Science), University of Texas MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
J Med Chem ; 64(20): 15141-15169, 2021 10 28.
Article in En | MEDLINE | ID: mdl-34643390
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Enzyme Inhibitors / Protein Tyrosine Phosphatase, Non-Receptor Type 11 / Drug Discovery / Antineoplastic Agents Limits: Animals / Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2021 Document type: Article Affiliation country: Country of publication:
Fulltext
Add to My VHL
Print
XML
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Enzyme Inhibitors / Protein Tyrosine Phosphatase, Non-Receptor Type 11 / Drug Discovery / Antineoplastic Agents Limits: Animals / Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2021 Document type: Article Affiliation country: Country of publication: