DC Chemicals · Product datasheet

APS-2-79 — Datasheet

CAT. NO. DC10048

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ParameterValue
Chemical Name6,7-Dimethoxy-~{n}-(2-Methyl-4-Phenoxy-Phenyl)quinazolin-4-Amine
CAS No.2002381-25-9
SynonymsAPS-2-79;APS 2-79;6,7-dimethoxy-N-(2-methyl-4-phenoxyphenyl)quinazolin-4-amine;6,7-Dimethoxy-~{n}-(2-Methyl-4-Phenoxy-Phenyl)quinazolin-4-Amine;BDBM429286;BCP24938;US10548897, Compound 21;Q27456559;COC=1C=C2C(=NC=NC2=CC=1OC)NC1=C(C=C(C=C1)OC1=CC=CC=C1)C;6U7
FormulaC23H21N3O3
M.Wt387.4311
SMILESO(C1C([H])=C([H])C([H])=C([H])C=1[H])C1C([H])=C([H])C(=C(C([H])([H])[H])C=1[H])N([H])C1C2=C([H])C(=C(C([H])=C2N=C([H])N=1)OC([H])([H])[H])OC([H])([H])[H]
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

APS-2-79 behaves as a kinase suppressor of Ras (KSR)-dependent antagonist of RAF-mediated MEK phosphorylation. APS-2-79 binds directly to KSR2 within the KSR2-MEK1 complex with an IC 50 of 120±23 nM for KSR2.

In Vitro

APS-2-79 (1 μM) shifts the cell viability dose response to Trametinib in Ras-mutant cell lines HCT-116 and A549, but not BRAF mutant cell lines SK-MEL-239 and A375. Although the cellular effects of APS-2-79 alone are modest, combination analysis over full concentration matrices reveal that kinase suppressor of Ras (KSR)-inactive state (KSRi) synergizes with Trametinib, and other MEK inhibitors, specifically in KRAS mutant cell lines. APS-3-77, and additional control compounds, do not demonstrate Ras-mutant-specific synergy, supporting the hypothesis that the enhanced activity of Trametinib when combined with APS-2-79 depends on co-modulation of KSR[1].

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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