Batoprotafib

Last updated

Batoprotafib
Batoprotafib.svg
Identifiers
  • (3S,4S)-8-[6-amino-5-(2-amino-3-chloropyridin-4-yl)sulfanylpyrazin-2-yl]-3-methyl-2-oxa-8-azaspiro[4.5]decan-4-amine
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
ChEMBL
PDB ligand
Chemical and physical data
Formula C18H24ClN7OS
Molar mass 421.95 g·mol−1
3D model (JSmol)
  • C[C@H]1[C@H](C2(CCN(CC2)C3=CN=C(C(=N3)N)SC4=C(C(=NC=C4)N)Cl)CO1)N
  • InChI=1S/C18H24ClN7OS/c1-10-14(20)18(9-27-10)3-6-26(7-4-18)12-8-24-17(16(22)25-12)28-11-2-5-23-15(21)13(11)19/h2,5,8,10,14H,3-4,6-7,9,20H2,1H3,(H2,21,23)(H2,22,25)/t10-,14+/m0/s1
  • Key:UCJZOKGUEJUNIO-IINYFYTJSA-N

Batoprotafib (TNO155) is an experimental drug which acts as a selective inhibitor of the protein tyrosine phosphatase enzyme SHP2, which regulates cell growth and differentiation through the MAPK signaling pathway. It is in early stage clinical trials against lung cancer, squamous cell carcinoma and peripheral nerve sheath tumors. [1] [2] [3] [4] [5] [6]

References

  1. ↑ LaMarche MJ, Acker M, Argintaru A, Bauer D, Boisclair J, Chan H, et al. (November 2020). "Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer". Journal of Medicinal Chemistry. 63 (22): 13578–13594. doi:10.1021/acs.jmedchem.0c01170. PMID   32910655.
  2. ↑ Wang J, Calizo A, Zhang L, Pino JC, Lyu Y, Pollard K, et al. (November 2023). "CDK4/6 inhibition enhances SHP2 inhibitor efficacy and is dependent upon RB function in malignant peripheral nerve sheath tumors". Science Advances. 9 (47) eadg8876. Bibcode:2023SciA....9G8876W. doi:10.1126/sciadv.adg8876. PMC   10672174 . PMID   38000020.
  3. ↑ Prahallad A, Weiss A, Voshol H, Kerr G, Sprouffske K, Yuan T, et al. (December 2023). "CRISPR Screening Identifies Mechanisms of Resistance to KRASG12C and SHP2 Inhibitor Combinations in Non-Small Cell Lung Cancer". Cancer Research. 83 (24): 4130–4141. doi:10.1158/0008-5472.CAN-23-1127. PMC   10722132 . PMID   37934115.
  4. ↑ Valencia-Sama I, Kee L, Christopher G, Ohh M, Layeghifard M, Shlien A, et al. (December 2023). "SHP2 Inhibition with TNO155 Increases Efficacy and Overcomes Resistance of ALK Inhibitors in Neuroblastoma". Cancer Research Communications. 3 (12): 2608–2622. doi:10.1158/2767-9764.CRC-23-0234. PMC   10752212 . PMID   38032104.
  5. ↑ Chai AW, Tan YH, Ooi S, Yee PS, Yee SM, Cheong SC (November 2024). "TNO155 is a selective SHP2 inhibitor to target PTPN11-dependent oral squamous cell carcinoma". Heliyon. 10 (21) e39677. Bibcode:2024Heliy..1039677C. doi: 10.1016/j.heliyon.2024.e39677 . PMC   11550046 . PMID   39524880.
  6. ↑ Oya Y, Imaizumi K, Mitsudomi T (August 2024). "The next-generation KRAS inhibitors…What comes after sotorasib and adagrasib?". Lung Cancer. 194 107886. doi: 10.1016/j.lungcan.2024.107886 . PMID   39047616.
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