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over3years
[VIRTUAL] DAY101, a potent pan-RAF inhibitor with activity in preclinical models harboring MAPK pathway alterations beyond BRAF V600E mutation (AACR 2021)
Accordingly, the tool compound TAK-632, which exhibits comparable biochemical and cellular potency to DAY101, was used alternatively as needed for in vitro assays.Single-agent anti-proliferative activity was observed in a melanoma BRAF fusion PDX model treated with TAK-632 ex vivo, with less sensitivity observed in models beyond melanoma harboring other BRAF fusions. Inhibition of both RAF monomers and dimers by DAY101 enables a broader indication selection strategy, beyond LGG and BRAF alterations. Ongoing translational work will highlight the potential utility of DAY101 in adult tumors harboring RAS or RAF alterations, both as a single agent and in hypothesis-driven combinations.
Preclinical
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KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • KIAA1549
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BRAF V600E • KRAS mutation • BRAF V600 • KIAA1549-BRAF fusion • BRAF fusion
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Ojemda (tovorafenib) • TAK‐632