APS-2-79 MedChemExpress (MCE)

Product Name	APS-2-79 (hydrochloride)
Synonyms	APS279;APS-279;CS-2444;APS-2-79;APS 2 79;APS-2-79 (hydrochloride);6,7-dimethoxy-N-(2-methyl-4-phenoxyphenyl)quinazolin-4-amine hydrochloride
CAS	2002381-31-7
EINECS
Chemical Formula	C23H22ClN3O3
Molecular Weight	423.9
inchi
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Descriptions	APS-2-79 hydrochloride APS-2-79 hydrochloride MedChemExpress (MCE) HY-100627A 2002381-31-7 Please store the product under the recommended conditions in the Certificate of Analysis. Room temperature in continental US Descriptions APS-2-79 hydrochloride APS-2-79 hydrochloride MedChemExpress (MCE) HY-100627A 2002381-31-7 Please store the product under the recommended conditions in the Certificate of Analysis. Room temperature in continental US may vary elsewhere. APS-2-79 hydrochloride is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATPbiotin binding to KSR2 within the KSR2-MEK1 complexe with an IC50 of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling. APS-2-79 (5 μM) suppresses KSR-stimulated MEK and ERK phosphorylation in 293H cells[1]. APS-2-79 (1 μM) enhances the efficacy of the clinical MEK inhibitor trametinib within cancer cell lines containing K-Ras mutations[1] Cell viability assays are performed in 96 well plates. Optimal cell densities for 96 well plate assays are determined to obtain linear growth over the time course of assays. A549, HCT-116, A375, SK-MEL-239, COLO-205, LOVO, SK-MEL-2, CALU-6, MEWO, SW620 and SW1417 cells are plated at 500 cells per well and treated with inhibitors (e.g., APS-2-79 100-3,000 nM) for 72hrs before measuring viability. H2087 and HEPG2 cells are plated at 2000 cells per well, and treated with inhibitors (e.g., APS-2-79 100-3,000 nM) for 72hrs. Cell viability is measured using Resazurin, and the percent cell viability is determined by normalizing inhibitor-treated samples to DMSO controls[1]. KSR2 120 nM (IC50) MEK1 \| \| \| \| \| \| \| \| \| \| [1]. Dhawan NS, et al. Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature. 2016 Sep 1 537(7618):112-116. [Content Brief]
Last Update	2025-04-01 14:45:47

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