TWG-07-148

Chemical Structure : TWG-07-148

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货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	627.41
分子式	C27H23FIN5O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

1. Sayan Chakraborty, et al. bioRxiv [Preprint]. 2025 Dec 17:2025.12.15.693503.

TWG-07-148

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TWG-07-148

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