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Pillar 1 - FTO (new thread), page-905

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    Great research @Jdlc.

    Based on what I can see when I compare the article you have shared and the City of Hope article, Bisantrene achieves a much better response in AML cells.

    I'll compare with some of the basic things that I have seen.

    Cell viability:
    SsD (left) = 400 - 2000 nM
    Bisantrene (CS1; right) = 22 - 175.9 nM

    https://hotcopper.com.au/data/attachments/3122/3122046-3f973eae78beace9de38075ac3afeaa7.jpghttps://hotcopper.com.au/data/attachments/3122/3122055-f2b091a8cc207bc1de03d3ad36fb4add.jpg


    Colony numbers:
    SsD (left) = 1 uM achieved significant reduction
    Bisantrene (right) = 50 nM almost completely abolished colony numbers
    https://hotcopper.com.au/data/attachments/3122/3122083-c730067a7e919911ea3d0516a8fb86fa.jpghttps://hotcopper.com.au/data/attachments/3122/3122136-8eb3bcae26be4499e091e6041442b34d.jpg

    FTO inhibition:
    SsD (left) = 460 nM
    Bisantrene (right) = 142 nM

    https://hotcopper.com.au/data/attachments/3122/3122153-ec7f1c1e2aa889f8b31b9c9b321eaf96.jpghttps://hotcopper.com.au/data/attachments/3122/3122149-fc434879f2113a489d48691ec8d3f68c.jpg


    Downstream Gene Expression:
    SsD = 1uM to get significant effect in MYC and RARA
    Bisantrene = 100 - 300 nM to achieve a significant effect in MYC and RARA

    https://hotcopper.com.au/data/attachments/3122/3122163-414c21645eb94710b9efefeb8a8c6ce4.jpg
    https://hotcopper.com.au/data/attachments/3122/3122177-2f8cb7f15e2785c2b3e3b47229664b4b.jpg

    Hence, less Bisantrene is required to achieve a response. Add in that this drug is at the very beginning of clinical development and is not clinically mature like Bisantrene, you then start to further appreciate the value of Bisantrene.
 
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