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.


Price and Availability

Size Price Shipping out time Quantity
100mg USD 450 2 Weeks
200mg USD 750 2 Weeks
500mg USD 1050 2 Weeks
1g USD 1950 2 Weeks
2g USD 2950 2 Weeks
5g USD 4250 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-31. Prices are subject to change without notice.

APS-2-79, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 406958
Name: APS-2-79
CAS#: 2002381-25-9
Chemical Formula: C23H21N3O3
Exact Mass: 387.1583
Molecular Weight: 387.439
Elemental Analysis: C, 71.30; H, 5.46; N, 10.85; O, 12.39


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


Technical Data

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


Additional Information

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.


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.