Chemical Structure : TWG-07-148
CAS No.:
2665700-96-7
TWG-07-148
Catalog No.: PC-25949Not For Human Use, Lab Use Only.
TWG-07-148 is a potent, covalent ARAF-MEK inhibitor with IC50 of 5.5 nM in biochemical ARAF-MEK assays, binds irreversibly to Cys514 on ARAF.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
TWG-07-148 is a potent, covalent ARAF-MEK inhibitor with IC50 of 5.5 nM in biochemical ARAF-MEK assays, binds irreversibly to Cys514 on ARAF.
TWG-07-148 more potently inhibits ARAF-MEK signaling as compared with trametinib and other existing MEK inhibitors.
TWG-07-148 dose-dependently suppresses MAP kinase pathway signaling in Ba/F3 cell models driven by BRAF S365A, CRAF S259A, and BRAF V600E.
TWG-07-148 inhibits proliferation of cancer cell lines driven by BRAF or KRAS mutations, with IC50 values ranging from 6 nM for A375 (BRAF V600E) to 81 nM in A549 (KRAS G12S).
TWG-07-148 inhibits phosphorylation of MEK and ERK in BRAF V600E+ melanoma cells lines A375 and HT29.
TWG-07-148 induces cell cycle arrest in RAF-mutant Ba/F3 cell lines and in BRAFV600E+ cancer cell lines.
Physicochemical Properties
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M.Wt
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627.41
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Formula
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C27H23FIN5O4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(3-(3-cyclopropyl-5-((2-fluoro-4-iodophenyl)amino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl)phenyl)acrylamide
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References
1. Sayan Chakraborty, et al. bioRxiv [Preprint]. 2025 Dec 17:2025.12.15.693503.
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