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S-63845

CAS No. 1799633-27-4

S-63845( S 63845 | S63845 )

Catalog No. M12723 CAS No. 1799633-27-4

S-63845 (S63845) is a highly potent, selective Mcl-1 inhibitor with Kd of 0.19 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    S-63845
  • Note
    Research use only, not for human use.
  • Brief Description
    S-63845 (S63845) is a highly potent, selective Mcl-1 inhibitor with Kd of 0.19 nM.
  • Description
    S-63845 (S63845) is a highly potent, selective Mcl-1 inhibitor with Kd of 0.19 nM, with no appreciable binding affinity to BCL-2 or BCL-XL (Ki>10 uM); binds to the BH3-binding groove of Mcl-1, potently kills MCL1-dependent cancer cells, including multiple myeloma (IC50<0.1 uM), leukaemia and lymphoma cells, by activating the BAX/BAK-dependent mitochondrial apoptotic pathway; is well tolerated and shopws high effectivity against mouse cancer models.Blood Cancer Preclinical.
  • In Vitro
    The pro-survival protein myeloid cell leukemia 1 (MCL1) is over expressed in many cancers. S63845 is a small molecule that specifically binds with high affinity to the BH3-binding groove of MCL1. S63845 potently kills MCL1-dependent cancer cells, including multiple myeloma, leukaemia and lymphoma cells, by activating the BAX/BAK-dependent mitochondrial apoptotic pathway. The activity of S63845 is next evaluated in a panel of eight AML cell lines: all lines are sensitive to S63845 (IC50=4-233 nM).
  • In Vivo
    S63845 shows potent anti-tumour activity with an acceptable safety margin as a single agent in several cancers. Intravenously injected (i.v.) S63845 exerts dose-dependent anti-tumour activity in human multiple myeloma (H929 and AMO1) xenografts in immunocompromised mice, with maximal tumour growth inhibition of 114% in the AMO1 model and 103% in the H929 model. At 25 mg/kg, S63845 induces complete regression in 7 out of 8 of the mice at 100 days after treatment in the AMO1 model.
  • Synonyms
    S 63845 | S63845
  • Pathway
    Angiogenesis
  • Target
    Bcl-2
  • Recptor
    Bcl-2
  • Research Area
    Cancer
  • Indication
    Blood cancer

Chemical Information

  • CAS Number
    1799633-27-4
  • Formula Weight
    829.2593
  • Molecular Formula
    C39H37ClF4N6O6S
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO
  • SMILES
    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
  • Chemical Name
    Dispiro[cyclohexane-1,2'-[2H]indene-1'(3'H),2''-[2H]imidazol]-4''-amine, 4-methoxy-5''-methyl-6'-[5-(1-propyn-1-yl)-3-pyridinyl]-, (1α,1'R,4β)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Kotschy A, et al. Nature. 2016 Oct 27;538(7626):477-482. 2. Merino D, et al. Sci Transl Med. 2017 Aug 2;9(401). pii: eaam7049. 3. Letai A. Cancer Cell. 2016 Dec 12;30(6):834-835.
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