Chemistry:BX-912

From HandWiki
BX-912
BX-912.svg
Names
Preferred IUPAC name
N-{3-[(5-Bromo-4-{[2-(1H-imidazol-5-yl)ethyl]amino}pyrimidin-2-yl)amino]phenyl}pyrrolidine-1-carboxamide
Identifiers
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
UNII
Properties
C20H23BrN8O
Molar mass 471.363 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references
Tracking categories (test):

BX-912 is a small molecule that inhibits 3-phosphoinositide dependent protein kinase-1.[1][2][3] The phosphoinositide 3-kinase/3-phosphoinositide-dependent kinase 1 (PDK1)/AKT signaling pathway plays a role in cancer cell growth, and tumor angiogenesis, and could be a new target for anti-cancer drugs.[4]

File:Tumor-Angiogenesis-and-Vascular-Patterning-A-Mathematical-Model-pone.0019989.s006.ogv

References

  1. Zimmermann, Yvonne; Giller, Vladimir; Zoellner, Anna-Katharina; Weigert, Oliver; Hiddemann, Wolfgang; Dreyling, Martin (2013-11-15). "High Efficiency Of the PDPK1-Inhibitor, BX912, In MCL". U.S.: Blood. pp. 3077. http://www.bloodjournal.org/content/122/21/3077. 
  2. Weber, David S; Sullivan, Lydia M; Bennett, Justin R; McCarthy, Cullen (2013-04-01). "Activation of PDK1 mediates VSMC migration and may contribute to vascular remodeling following injury". The FASEB Journal 27: 922.10. doi:10.1096/fasebj.27.1_supplement.922.10. 
  3. Maegawa, Saori; Chinen, Yoshiaki; Shimura, Yuji; Tanba, Kazuna; Takimoto, Tomoko; Mizuno, Yoshimi; Matsumura-Kimoto, Yayoi; Kuwahara-Ota, Saeko et al. (2018-03-01). "Phosphoinositide-dependent protein kinase 1 is a potential novel therapeutic target in mantle cell lymphoma". Experimental Hematology (ScienceDirect) 59: 72–81.e2. doi:10.1016/j.exphem.2017.12.006. PMID 29287939. 
  4. Feldman, Richard I.; Wu, James M.; Polokoff, Mark A.; Kochanny, Monica J.; Dinter, Harald; Zhu, Daguang; Biroc, Sandra L.; Alicke, Bruno et al. (2005-05-20). "Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1". The Journal of Biological Chemistry 280 (20): 19867–19874. doi:10.1074/jbc.M501367200. ISSN 0021-9258. PMID 15772071.