Tunlametinib | MEK inhibitor | Probechem Biochemicals

Chemical Structure : Tunlametinib

CAS No.: 1801756-06-8

Tunlametinib (HL-085, HL085)

Catalog No.: PC-38424Not For Human Use, Lab Use Only.

Tunlametinib (HL-085) is a highly selective and potent MEK inhibitor with IC50 of 1.9 nM (MEK1), exhibits potent activity against RAS/RAF mutant cancer cells.

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Biological Activity

Tunlametinib (HL-085) is a highly selective and potent MEK inhibitor with IC50 of 1.9 nM (MEK1), exhibits potent activity against RAS/RAF mutant cancer cells.

Tunlametinib (HL-085) exhibits approximately 19-fold greater inhibitory activity against MEK1/MAP2K1(h) kinase than the lead compound MEK162.

Tunlametinib (HL-085) at 10 μmol/L shows complete inhibition against MEK1 and no inhibition against other 77 kinases tested.

Tunlametinib (HL-085) dramatically inhibits cell proliferation in a panel of cell lines with RAS or RAF mutation, with IC50 values of 0.67 and 59.89 nM, with minimal inhibitory effect on the proliferation of RAS/RAF wild-type tumor cells (H1975) and normal cells (MRC-5)

Tunlametinib (HL-085) is more effective for RAS/RAF-mutant cell lines with improved potency compared to AZD6244.

Tunlametinib (HL-085) potently inhibits ERK phosphorylation in A375 cells with IC50 of 1.16 nM.

Tunlametinib (HL-085) could dose-dependently increase the proportion of G0/G1 phase in A375 cells at concentration from 1 nM to 9 nM.

Tunlametinib (HL-085) (1, 3, 6 mg/kg, QD) inhibits tumor growth of cell line-derived xenografts (CDXs) or patient derived CRC xenograft (PDX).

Tunlametinib (HL-085) combined with BRAF/KRASG12C/SHP2 inhibitors or docetaxel showed synergistically enhanced response and marked tumor inhibition.

Physicochemical Properties

M.Wt	491.251
Formula	C16H12F2IN3O3S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-fluoro-5-((2-fluoro-4-iodophenyl)amino)-N-(2-hydroxyethoxy)benzo[d]thiazole-6-carboxamide

References

1. Patent WO2013107283 A1.
2. Liu Y, et al. Front Pharmacol. 2023 Sep 21;14:1271268.

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Tunlametinib (HL-085, HL085)

Biological Activity

Physicochemical Properties

References

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