2. Academic Validation
  3. Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms

Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms

  • ACS Med Chem Lett. 2015 Jul 12;6(8):850-5. doi: 10.1021/acsmedchemlett.5b00226.
Honghe Wan 1,  Gretchen M Schroeder 1,  Amy C Hart 1,  Jennifer Inghrim 1,  James Grebinski 1,  John S Tokarski 1,  Matthew V Lorenzi 1,  Dan You 1,  Theresa Mcdevitt 1,  Becky Penhallow 1,  Ragini Vuppugalla 1,  Yueping Zhang 1,  Xiaomei Gu 1,  Ramaswamy Iyer 1,  Louis J Lombardo 1,  George L Trainor 1,  Stefan Ruepp 1,  Jonathan Lippy 1,  Yuval Blat 1,  John S Sack 1,  Javed A Khan 1,  Kevin Stefanski 1,  Bogdan Sleczka 1,  Arvind Mathur 1,  Jung-Hui Sun 1,  Michael K Wong 1,  Dauh-Rurng Wu 1,  Peng Li 1,  Anuradha Gupta 1,  P N Arunachalam 1,  Bala Pragalathan 1,  Sankara Narayanan 1,  Nanjundaswamy K C 1,  Prakasam Kuppusamy 1,  Ashok V Purandare 1
Affiliations

Affiliation

  • 1 Bristol-Myers Squibb R&D , US Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, United States.
PMID: 26288683 DOI: 10.1021/acsmedchemlett.5b00226
Abstract

JAK2 kinase inhibitors are a promising new class of agents for the treatment of myeloproliferative neoplasms and have potential for the treatment of Other Diseases possessing a deregulated JAK2-STAT pathway. X-ray structure and ADME guided refinement of C-4 heterocycles to address metabolic liability present in dialkylthiazole 1 led to the discovery of a clinical candidate, BMS-911543 (11), with excellent kinome selectivity, in vivo PD activity, and safety profile.

Keywords

BMS-911543; JAK2; myeloproliferative neoplasm; selective inhibitor; structure-guided design.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-15270
    98.53%, JAK 抑制剂
    JAK
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