Excellent work once again @Boffin99
Just a minor correction, which I've shamelessly grabbed the opportunity to point out, and to provide some context for newer readers.
Point 3 remains an extremely good indicator for Zantrene - although not because FB23-2 has a lower IC50 value, but because FB23-2 has a higher IC50 value than Zantrene.
As Zantrene exhibits, by some distance, a much lower IC50 than FB23-2 then it means much less Zantrene is needed to achieve the same effect.
In other words, Zantrene is much more potent than FB23-2.
For those new to the Zantrene story, with regard to potency, keep in mind that:
- City of Hope in Los Angeles recognised that FTO is a huge therapeutic target, and consequently....
- They independently screened over 260,000 compounds as potential inhibitors of FTO and arrived at two (repeat, '2') compounds worthy of further studies.
- They called them 'CS1' and 'CS2' (https://www.sciencedirect.com/science/article/pii/S0006497118581519)
- 'CS1' was shown to have an IC50 of 142.6nM (https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8496078/)
- 'CS2' was shown to have an IC50 of 712.8nM (approx 5 times less potent than 'CS1')
- When considering the therapeutic effects, this is what City of Hope found after comparing CS1, CS2 and FB23-2 (https://www.sciencedirect.com/science/article/pii/S0006497118581519). They even helpfully referenced the relative potencies in the context of anti-AML efficacy.
- City of Hope must have thought 'CS1' was awesome; they tried to develop analogues of it (and that was even without the radiotherapy considerations that @Boffin99 is pointing out).
- They couldn't - it turns out 'CS1' and analogues is already patented
- By Race Oncology
- 'CS1' is otherwise known as 'Bisantrene' (https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8496078/)
- 'Bisantrene' is otherwise known as 'Zantrene'
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