Chemistry:Avutometinib
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Short description: Chemical compound
Skeletal formula and ball-and-stick model of avutometinib | |
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Other names | RO-5126766; CH-5126766; CKI-27; R-7304; RG-7304 |
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Elimination half-life | 60 h (45.8–93.7 h) |
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Formula | C21H18FN5O5S |
Molar mass | 471.46 g·mol−1 |
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Avutometinib (INN; codenamed RO-5126766, CH-5126766, CKI-27, R-7304, RG-7304, and VS-6766 at various stages of its development) is an inhibitor of Ras-Raf-MEK-ERK signaling being developed as a potential treatment for cancer.
It was discovered by Chugai Pharmaceutical Co. (a subsidiary of Roche) through derivatization of a hit compound identified by high-throughput screening.[1] It was licensed by Verastem Oncology in 2020 for clinical trials.[2][3]
References
- ↑ "Enhanced inhibition of ERK signaling by a novel allosteric MEK inhibitor, CH5126766, that suppresses feedback reactivation of RAF activity". Cancer Res 73 (13): 4050–4060. July 2013. doi:10.1158/0008-5472.CAN-12-3937. PMID 23667175.
- ↑ Adams, Ben (2020-01-08). "Verastem pens KRAS-focused drug licensing deal with Chugai". Fierce Biotech. https://www.fiercebiotech.com/biotech/verastem-pens-kras-focused-drug-licence-deal-chugai-pharmaceutical. Retrieved 2022-06-05.
- ↑ "Drug Profile: Avutometinib " (PDF). AdisInsight. 2022-05-23. https://adisinsight.springer.com/drugs/800029782. Retrieved 2022-06-05.
Original source: https://en.wikipedia.org/wiki/Avutometinib.
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