BX-912
Appearance
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Preferred IUPAC name
N-{3-[(5-Bromo-4-{[2-(1H-imidazol-5-yl)ethyl]amino}pyrimidin-2-yl)amino]phenyl}pyrrolidine-1-carboxamide | |
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3D model (JSmol)
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ChEBI | |
ChEMBL | |
ChemSpider | |
ECHA InfoCard | 100.237.653 |
PubChem CID
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UNII | |
CompTox Dashboard (EPA)
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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).
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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]
References
[edit]- ^ 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". Blood. U.S.: Blood. p. 3077. Retrieved 2019-09-29.
- ^ 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.
- ^ Maegawa, Saori; Chinen, Yoshiaki; Shimura, Yuji; Tanba, Kazuna; Takimoto, Tomoko; Mizuno, Yoshimi; Matsumura-Kimoto, Yayoi; Kuwahara-Ota, Saeko; Tsukamoto, Taku (2018-03-01). "Phosphoinositide-dependent protein kinase 1 is a potential novel therapeutic target in mantle cell lymphoma". Experimental Hematology. 59. ScienceDirect: 72–81.e2. doi:10.1016/j.exphem.2017.12.006. PMID 29287939.
- ^ Feldman, Richard I.; Wu, James M.; Polokoff, Mark A.; Kochanny, Monica J.; Dinter, Harald; Zhu, Daguang; Biroc, Sandra L.; Alicke, Bruno; Bryant, Judi (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. S2CID 7140790.