An inhibitor of KSR-dependent MAPK signaling
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APS-2-79 (hydrochloride)

Item No. 22137

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6,7-dimethoxy-N-(2-methyl-4-phenoxyphenyl)-4-quinazolinamine, monohydrochloride
CAS Number
2002381-31-7
Molecular Formula
C23H21N3O3 • HCl
Formula Weight
423.9
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 25 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.3 mg/mlEthanol: 1 mg/ml
λmax
220, 252, 342 nm
SMILES
COC1=C(OC)C=C(C(NC2=C(C)C=C(OC3=CC=CC=C3)C=C2)=NC=N4)C4=C1.Cl
InChi Code
InChI=1S/C23H21N3O3.ClH/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);1H
InChi Key
LIXKSHWZJNNZHG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    25 mg

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    Cayman Chemical
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    Product Description

    APS-2-79 is an inhibitor of MAPK signaling dependent on kinase suppressor of Ras (KSR).1 It inhibits ATPbiotin binding to KSR2 in KSR2-MEK1 complexes (IC50 = 120 nM), stabilizes KSR2 in an inactive state, and reduces interactions between B-RAF and KSR2-MEK1 complexes.1,2 APS-2-79 (5 μM) inhibits KSR-stimulated phosphorylation of MEK and ERK in HEK293H cells.1 It enhances the efficacy of the MEK inhibitor trametinib (Item No. 16292), further reducing cell viability in HCT116 and A549 cell lines containing K-Ras mutations, but not B-RAF mutant SK-MEL-239 and A375 cell lines, when used at a concentration of 1 μM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dhawan, N.S., Scopton, A.P., and Arvin, C.D. Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature 537(7618), 112-116 (2016).

    2. Neilsen, B.K., Frodyma, D.E., Lewis, R.E., et al. KSR as a therapeutic target for Ras-dependent cancers. Expert Opin. Ther. Targets. 21(5), 499-509 (2017).