APS-2-79
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MedKoo CAT#: 406958

CAS#: 2002381-25-9

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.


Chemical Structure

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APS-2-79
CAS# 2002381-25-9

Theoretical Analysis

MedKoo Cat#: 406958
Name: APS-2-79
CAS#: 2002381-25-9
Chemical Formula: C23H21N3O3
Exact Mass: 387.16
Molecular Weight: 387.439
Elemental Analysis: C, 71.30; H, 5.46; N, 10.85; O, 12.39

Price and Availability

Size Price Availability Quantity
100mg USD 450
200mg USD 750
500mg USD 1050
1g USD 1950
2g USD 2950
5g USD 4250
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Synonym: APS-2-79; APS 2-79; APS2-79; APS-279; APS 279; APS279.

IUPAC/Chemical Name: 6,7-Dimethoxy-N-(2-methyl-4-phenoxyphenyl)quinazolin-4-amine

InChi Key: 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 Code: CC1=CC(OC2=CC=CC=C2)=CC=C1NC3=C4C=C(OC)C(OC)=CC4=NC=N3

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Deregulation of the Ras-mitogen activated protein kinase (MAPK) pathway is an early event in many different cancers and a key driver of resistance to targeted therapies. Sustained signalling through this pathway is caused most often by mutations in K-Ras, which biochemically favours the stabilization of active RAF signalling complexes. Kinase suppressor of Ras (KSR) is a MAPK scaffold that is subject to allosteric regulation through dimerization with RAF. Direct targeting of KSR could have important therapeutic implications for cancer.

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 387.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.