bs-6512C

DATASHEET

Formulation Powder

Storage: Store in dry, dark place at -20C for 1 year.

Product Information:

Molecular Weight: 387.43

Formula: C23 H21 N3 O3

CAS Number: 2002381-25-9

InChi Key: PEKZLFZZBGBOPJ-UHFFFAOYSA-N

InChi: 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: CC1C=C(C=CC=1NC1=NC=NC2=CC(OC)=C(C=C21)OC)OC1C=CC=CC=1

Purity: 98.0

Solubility: Soluble in DMSO

Appearance: Solid Power

Shelf Life: 1.0 years

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.