Product Data Sheet

Tunlametinib (HL-085)

Catalog No. A24217

main product photo
Tunlametinib is a highly selective, orally active MEK1/2 inhibitor with an IC50 of 1.9 nM against MEK1. It effectively blocks the RAS-RAF-MEK-ERK signaling cascade, inducing cell cycle arrest and apoptosis. Tunlametinib exhibits strong antiproliferative activity against RAS/RAF mutant cancer cells, including BRAF^V600E and KRAS^G12C mutants, and shows synergistic anti-tumor effects when combined with BRAF, KRAS^G12C, or SHP2 inhibitors, as well as Docetaxel. It is a promising agent for the study of targeted therapies in RAS/RAF-driven malignancies such as melanoma, colorectal cancer, and non-small cell lung cancer.
Chemical Information
Catalog NumA24217
M. Wt491.25
FormulaC16H12F2IN3O3S
Purity>98%
Storageat -20 °C 3 years (powder form); at -20 °C 6 months (Solution base)
CAS No.1801756-06-8
Synonyms
SMILESO=C(C1=CC2=C(C(F)=C1NC3=CC=C(C=C3F)I)N=CS2)NOCCO
Biological Activity
DescriptionTunlametinib is a highly selective, orally active MEK1/2 inhibitor with an IC50 of 1.9 nM against MEK1. It effectively blocks the RAS-RAF-MEK-ERK signaling cascade, inducing cell cycle arrest and apoptosis. Tunlametinib exhibits strong antiproliferative activity against RAS/RAF mutant cancer cells, including BRAF^V600E and KRAS^G12C mutants, and shows synergistic anti-tumor effects when combined with BRAF, KRAS^G12C, or SHP2 inhibitors, as well as Docetaxel. It is a promising agent for the study of targeted therapies in RAS/RAF-driven malignancies such as melanoma, colorectal cancer, and non-small cell lung cancer.
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