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Sapanisertib

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Chemical compound Pharmaceutical compound
Sapanisertib
Identifiers
IUPAC name
  • 5-(4-Amino-1-propan-2-ylpyrazolopyrimidin-3-yl)-1,3-benzoxazol-2-amine
CAS Number
PubChem CID
UNII
KEGG
ChEBI
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC15H15N7O
Molar mass309.333 g·mol
3D model (JSmol)
SMILES
  • CC(C)N1C2=C(C(=N1)C3=CC4=C(C=C3)OC(=N4)N)C(=NC=N2)N
InChI
  • InChI=1S/C15H15N7O/c1-7(2)22-14-11(13(16)18-6-19-14)12(21-22)8-3-4-10-9(5-8)20-15(17)23-10/h3-7H,1-2H3,(H2,17,20)(H2,16,18,19)
  • Key:GYLDXIAOMVERTK-UHFFFAOYSA-N

Sapanisertib (also known as MLN0128, INK128 and TAK-228) is an experimental small molecule inhibitor of mTOR which is administered orally. It targets both mTORC1 and mTORC2.

Developed by Millennium Pharmaceuticals, and is in phase II clinical trials for breast cancer, endometrial cancer, glioblastoma, renal cell carcinoma, and thyroid cancer. The drug has been well tolerated by patients with advanced solid tumours in Phase I trials.

References

  1. Panchal II, Badeliya SN, Patel R, Patel A, Devaligar A (2019). "In silico Analysis and Molecular Docking Studies of Novel 4-Amino-3- (Isoquinolin-4-yl)-1H-PyrazoloPyrimidine Derivatives as Dual PI3-K/mTOR Inhibitors". Current Drug Discovery Technologies. 16 (3): 297–306. doi:10.2174/1568009618666181102144934. PMID 30387396. S2CID 54344624.
  2. Guo N, Azadniv M, Coppage M, Nemer M, Mendler J, Becker M, Liesveld J (April 2019). "Effects of Neddylation and mTOR Inhibition in Acute Myelogenous Leukemia". Translational Oncology. 12 (4): 602–613. doi:10.1016/j.tranon.2019.01.001. PMC 6348338. PMID 30699367.
  3. Ouvry G, Clary L, Tomas L, Aurelly M, Bonnary L, Borde E, et al. (November 2019). "Impact of Minor Structural Modifications on Properties of a Series of mTOR Inhibitors". ACS Medicinal Chemistry Letters. 10 (11): 1561–1567. doi:10.1021/acsmedchemlett.9b00401. PMC 6862343. PMID 31749911.
  4. Arnold A, Yuan M, Price A, Harris L, Eberhart CG, Raabe EH (April 2020). "Synergistic activity of mTORC1/2 kinase and MEK inhibitors suppresses pediatric low-grade glioma tumorigenicity and vascularity". Neuro-Oncology. 22 (4): 563–574. doi:10.1093/neuonc/noz230. PMC 7158655. PMID 31841591.
  5. "Sapanisertib - Takeda Oncology". Adis Insight. Springer Nature Switzerland AG.
  6. Moore KN, Bauer TM, Falchook GS, Chowdhury S, Patel C, Neuwirth R, et al. (February 2018). "Phase I study of the investigational oral mTORC1/2 inhibitor sapanisertib (TAK-228): tolerability and food effects of a milled formulation in patients with advanced solid tumours". ESMO Open. 3 (2): e000291. doi:10.1136/esmoopen-2017-000291. PMC 5812400. PMID 29464110.
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