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S-63845

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SKU: C-1370-5mg
C39H37ClF4N6O6S Solid powder
$149.99
  • Catalog#: C-1370
  • Synonym: S-63845; S63845; S 63845
  • Chemical Name/IUPAC:(R)-2-((5-(3-chloro-2-methyl-4-(2-(4-methylpiperazin-1-yl)ethoxy)phenyl)-6-(5-fluorofuran-2-yl)thieno[2,3-d]pyrimidin-4-yl)oxy)-3-(2-((1-(2,2,2-trifluoroethyl)-1H-pyrazol-5-yl)methoxy)phenyl)propanoic acid
  • SMILES Code: O=C(O)[C@@H](CC1=C(OCC2=CC=NN2CC(F)(F)F)C=CC=C1)OC3=C4C(SC(C5=CC=C(F)O5)=[C@@]4[C@@]6=C(C)C(Cl)=C(OCCN7CCN(C)CC7)C=C6)=NC=N3
    Technical Data
  • Product Name: S-63845
  • Chemical Formula: C39H37ClF4N6O6S
  • Molecular Weight: 829.26
  • CAS#: 1799633-27-4
  • Purity: > 99% by HPLC
  • Solubility: Soluble in DMSO
  • Storage: Room temperature for months, or -20ºC for 3 years
    Description
    S-63845 is a potent and selective MCL1 inhibitor (Ki (MCL1, FP) 10.000 1.2 nM; Ki (BCL-XL, FP) > 10.000 1.2 nM). S63845 specifically binds with high affinity to the BH3-binding groove of MCL1. S-63845 potently kills MCL1-dependent cancer cells, including multiple myeloma, leukaemia and lymphoma cells, by activating the BAX/BAK-dependent mitochondrial apoptotic pathway. In vivo, S63845 shows potent anti-tumour activity with an acceptable safety margin as a single agent in several cancers. Moreover, MCL1 inhibition, either alone or in combination with other anti-cancer drugs, proved effective against several solid cancer-derived cell lines. These results point towards MCL1 as a target for the treatment of a wide range of tumours.