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Chemical Structure| 2002381-31-7 Chemical Structure| 2002381-31-7

Structure of APS-2-79 HCl
CAS No.: 2002381-31-7

Chemical Structure| 2002381-31-7

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APS-2-79 HCl is a KSR (Kinase suppressor of Ras)-dependent MAPK modulator which can stabilize KSR inactive state with an IC50 value of 120 nM, resulting in inhibition of oncogenic Ras signaling, antagonizing the Ras–MAPK pathway.

Synonyms: APS-2-79 (hydrochloride); APS-2-79 HCl

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Product Details of APS-2-79 HCl

CAS No. :2002381-31-7
Formula : C23H22ClN3O3
M.W : 423.89
SMILES Code : CC1=CC(OC2=CC=CC=C2)=CC=C1NC3=C4C=C(OC)C(OC)=CC4=NC=N3.[H]Cl
Synonyms :
APS-2-79 (hydrochloride); APS-2-79 HCl
InChI Key :LIXKSHWZJNNZHG-UHFFFAOYSA-N
Pubchem ID :122177134

Safety of APS-2-79 HCl

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H302-H361-H372-H410
Precautionary Statements:P201-P264-P280-P301+P330+P331-P312
Class:9
UN#:3077
Packing Group:

Related Pathways of APS-2-79 HCl

MAPK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
SK-MEL-239 cells 1μM 48 h APS-2-79 does not enhance trametinib's inhibition in RAF-mutant cells PMC5161575
A549 cells 1μM 48 h APS-2-79 enhances trametinib's inhibition of ERK phosphorylation PMC5161575
HCT-116 cells 1μM 48 h APS-2-79 enhances trametinib's inhibition of ERK phosphorylation PMC5161575
293H cells 5μM 2 h APS-2-79 inhibits KSR-stimulated MAPK signaling PMC5161575
SKMEL2 cells 5 μM 2 h Evaluate the inhibitory effect of APS-2-79 on KSR1-bound ERK phosphorylation, results showed APS-2-79 could not prevent incorporation of phosphorylated ERK on KSR1 C809Y PMC9931222
HEK293T cells 5 μM 2 h Evaluate the inhibitory effect of APS-2-79 on KSR1-bound ERK phosphorylation, results showed APS-2-79 could not prevent incorporation of phosphorylated ERK on KSR1 C809Y PMC9931222

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Zebrafish Wild-type zebrafish Aqueous solution treatment 5 μM Single treatment, continuous observation Inhibition of KSR2 activity, leading to decreased sleep during both day and night PMC6853770

Protocol

Bio Calculators
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2.36mL

0.47mL

0.24mL

11.80mL

2.36mL

1.18mL

23.59mL

4.72mL

2.36mL

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