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Voxtalisib

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Chemical compound Pharmaceutical compound
Voxtalisib
Identifiers
IUPAC name
  • 2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)pyridopyrimidin-7-one
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEBI
ChEMBL
Chemical and physical data
FormulaC13H14N6O
Molar mass270.296 g·mol
3D model (JSmol)
SMILES
  • CCN1C2=NC(=NC(=C2C=C(C1=O)C3=CC=NN3)C)N
InChI
  • InChI=1S/C13H14N6O/c1-3-19-11-8(7(2)16-13(14)17-11)6-9(12(19)20)10-4-5-15-18-10/h4-6H,3H2,1-2H3,(H,15,18)(H2,14,16,17)
  • Key:RGHYDLZMTYDBDT-UHFFFAOYSA-N

Voxtalisib (XL-765, SAR245409) is a drug which acts as a dual inhibitor of the kinase enzymes phosphatidylinositol 3-kinase (PI3K) and mechanistic target of rapamycin (mTOR). It is in clinical trials for the treatment of various types of cancer.

References

  1. Prasad G, Sottero T, Yang X, Mueller S, James CD, Weiss WA, et al. (April 2011). "Inhibition of PI3K/mTOR pathways in glioblastoma and implications for combination therapy with temozolomide". Neuro-Oncology. 13 (4): 384–92. doi:10.1093/neuonc/noq193. PMC 3064692. PMID 21317208.
  2. Gravina GL, Mancini A, Scarsella L, Colapietro A, Jitariuc A, Vitale F, et al. (January 2016). "Dual PI3K/mTOR inhibitor, XL765 (SAR245409), shows superior effects to sole PI3K or mTOR inhibition in prostate cancer cell models". Tumour Biology. 37 (1): 341–51. doi:10.1007/s13277-015-3725-3. PMID 26219891. S2CID 23993969.
  3. Brown JR, Hamadani M, Hayslip J, Janssens A, Wagner-Johnston N, Ottmann O, et al. (April 2018). "Voxtalisib (XL765) in patients with relapsed or refractory non-Hodgkin lymphoma or chronic lymphocytic leukaemia: an open-label, phase 2 trial". The Lancet. Haematology. 5 (4): e170 – e180. doi:10.1016/S2352-3026(18)30030-9. PMC 7029813. PMID 29550382.
  4. Rehan M (2019). "Anticancer compound XL765 as PI3K/mTOR dual inhibitor: A structural insight into the inhibitory mechanism using computational approaches". PLOS ONE. 14 (6): e0219180. Bibcode:2019PLoSO..1419180R. doi:10.1371/journal.pone.0219180. PMC 6597235. PMID 31247018.
  5. Tarantelli C, Lupia A, Stathis A, Bertoni F (February 2020). "Is There a Role for Dual PI3K/mTOR Inhibitors for Patients Affected with Lymphoma?". International Journal of Molecular Sciences. 21 (3): 1060. doi:10.3390/ijms21031060. PMC 7037719. PMID 32033478.
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