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MEK&P38 MAPK

APS-2-79 (2002381-31-7)

APS-2-79 is an antagonist of MEK phosphorylation by RAF through direct binding of the KSR active site.

Not Intended for Therapeutic Use. For research use only.

CAS: 2002381-31-7 Category

APS-2-79 (2002381-31-7) Description:

APS-2-79 is a KSR-dependent MAPK modulator. APS-2-79 modulates KSR-dependent MAPK signalling by antagonizing RAF heterodimerization as well as the conformational changes required for phosphorylation and activation of KSR-bound MEK (mitogen-activated protein kinase kinase). APS-2-79 increased the potency of several MEK inhibitors specifically within Ras-mutant cell lines by antagonizing release of negative feedback signalling, demonstrating the potential of targeting KSR to improve the efficacy of current MAPK inhibitors. Co-targeting of enzymatic and scaffolding activities within Ras-MAPK signalling complexes is a therapeutic strategy for overcoming Ras-driven cancers.

APS-2-79 (2002381-31-7) Specifications:

Product Name APS-2-79
Synonym APS-2-79; APS 2-79; APS2-79; APS-279; APS 279; APS279.
Chemical Name 6,7-Dimethoxy-N-(2-methyl-4-phenoxyphenyl)quinazolin-4-amine
Drug Class N/A
Purity >98% (or refer to the Certificate of Analysis)
CAS Number 2002381-25-9
Molecular Formula C23H21N3O3
Molecular Weight 387.439
Monoisotopic Mass
387.158 g/mol

 

MDL number N/A
InChIKey PEKZLFZZBGBOPJ-UHFFFAOYSA-N
InChi Code InChI=1S/C23H21N3O3/c1-15-11-17(29-16-7-5-4-6-8-16)9-10-19(15)26-23-18-12-21(27-2)22(28-3)13-20(18)24-14-25-23/h4-14H,1-3H3,(H,24,25,26)
SMILES CC1=CC(OC2=CC=CC=C2)=CC=C1NC3=C4C=C(OC)C(OC)=CC4=NC=N3
Form solid powder
Color N/A
Solubility  Soluble in DMSO
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application APS-2-79 hydrochloride behaves as a kinase suppressor of Ras (KSR)-dependent antagonist of RAF-mediated MEK phosphorylation.

 

 


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RIDADR NONH for all modes of transport

References:

  • 1: KSR Mutations Guide Development of RAS Pathway Antagonists. Cancer Discov. 2016 Oct;6(10):1079. PubMed PMID: 27591198.
  • 2: Dhawan NS, Scopton AP, Dar AC. Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature. 2016 Aug 24;537(7618):112-116. doi: 10.1038/nature19327. [Epub ahead of print] PubMed PMID: 27556948.
  • 3.Dhawan NS, et al. Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature. 2016 Sep 1;537(7618):112-116.
  • 4.KSR as a therapeutic target for Ras-dependent cancers. Neilsen BK, Frodyma DE, Lewis RE, Fisher KW. Expert Opin Ther Targets. 2017 May;21(5):499-509. doi: 10.1080/14728222.2017.1311325. Epub 2017 Apr 7. Review.
  • 5.Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Dhawan NS, Scopton AP, Dar AC. Nature. 2016 Sep 1;537(7618):112-116. doi: 10.1038/nature19327. Epub 2016 Aug 24.

1 review for APS-2-79 (2002381-31-7)

  1. Cofttek

    Never had such good experience before,The APS-2-79 (2002381-31-7) is high purity,also customer service is pretty nice !gotta try!!

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