MELK-8a (hydrochloride)

产品描述：MELK-8a hydrochloride is a novel maternal embryonic leucine zipper kinase (MELK) inhibitor with an IC₅₀ of 2 nM. IC50 & Target: IC50: 2 nM (MELK)^[1] In Vitro: MELK-8a remains very potent (IC₅₀=140 nM) when the ATP concentration in the biochemical assay is shifted from 20 μM to 2 mM. Its potency is well tracked between full-length MELK versus catalytic domain construct (5 nM versus 2 nM). It only inhibits seven off-target kinases in addition to MELK with >85% inhibition of binding at 1 μM demonstrating great selectivity. The compound is at least 90-fold more selective in targeting MELK in all cases. MELK-8a is fairly soluble (0.22 g/L at pH 6.8) and shows a good permeability in the Caco-2 assay. MELK-8a inhibits the growth of MDA-MB-468 cells and MCF-7 cells with an IC₅₀ of approximately 0.06 and 1.2 μM, respectively^[1]. In Vivo: Subcutaneous administration of MELK-8a at 30 mg/kg in C57


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