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APS-2-79 hydrochloride

  Cat. No.:  DC9808   Featured
Chemical Structure
2002381-31-7
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Field of application
APS-2-79 is a novel modulator of KSR-dependent MAPK signalling,KSR2,IC50=120 nM
Cas No.: 2002381-31-7
Chemical Name: APS-2-79 hydrochloride
Synonyms: APS-2-79 (hydrochloride);APS 2-79 hydrochloride;6,7-Dimethoxy-N-(2-methyl-4-phenoxyphenyl)quinazolin-4-amine hydrochloride;APS279 hydrochloride;BCP23567;s8355;AK685587;6,7-dimethoxy-N-(2-methyl-4-phenoxyphenyl)quinazolin-4-amine HCl;APS-2-79 hydrochloride
SMILES: Cl[H].O(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]
Formula: C23H22ClN3O3
M.Wt: 423.8921
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: APS-2-79 hydrochloride 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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC7488 RO4987655 RO4987655(CH-4987655) is an orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1/MEK1 IC50=5.2 nM), with potential antineoplastic activity.
DC8473 Vacquinol-1 Vacquinol-1 is an activator of MKK4-dependent macropinocytotic cell death in glioblastoma cells.
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DC1099 Trametinib Trametinib is a highly specific and potent MEK1 and MEK2 inhibitor with IC50 of 0.92 nM and 1.8 nM, respectively.
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DC4177 Cobimetinib(GDC-0973; XL518) GDC-0973 is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase, also known as MEK, a serine/threonine kinase that is a component of the RAS/RAF/MEK/ERK pathway.
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