2. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK JAK/STAT Signaling PI3K/Akt/mTOR
  3. NEKs CDK Discoidin Domain Receptor EGFR PI3K
  4. AP4-43

AP4-43 is an orally active CLK1, CLK4, PI3K, DDR1, EGFR and NEK4 inhibitor. AP4-43 reduces growth of mammalian colorectal cancer organoids. AP4-43 improves survival in a transgenic Drosophila model of KRAS-mutant colorectal cancer. AP4-43 can be used for the research of KRAS-mutant colorectal cancer.

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AP4-43

AP4-43 Chemical Structure

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AP4-43 Related Antibodies

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Description

AP4-43 is an orally active CLK1, CLK4, PI3K, DDR1, EGFR and NEK4 inhibitor. AP4-43 reduces growth of mammalian colorectal cancer organoids. AP4-43 improves survival in a transgenic Drosophila model of KRAS-mutant colorectal cancer. AP4-43 can be used for the research of KRAS-mutant colorectal cancer[1].

IC50 & Target[1]

CLK1

 

CLK4

 

NEK4

 

DDR1

 

In Vitro

AP4-43 (10 pM-100 μM; 72 hr) inhibits the viability of SW620 human KRAS-driven colorectal cancer cells with an IC50 of 2.23 µM and SW837 cells with an IC50 of 15.41 µM[1].
AP4-43 (2 µM) reduces the growth of AKP mouse KRAS-mutant colorectal cancer organoids more effectively than 2 µM Regorafenib (HY-10331)[1].
AP4-43 (2 µM; 24 hr) inhibits CLK1-dependent Wnt/β-catenin signalling and CLK4-dependent NF-κB activation in AKP mouse KRAS-mutant colorectal cancer organoids, without affecting PI3K-AKT or RAS-MAPK pathway activity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AP4-43 Related Antibodies

Cell Viability Assay[1]

Cell Line: SW620 and SW837 cell lines
Concentration: 10 pM; 100 pM; 1 nM; 10 nM; 100 nM; 1 μM; 10 μM; 100 μM
Incubation Time: 72 h
Result: Inhibited the viability of SW620 human KRAS-driven colorectal cancer cells and SW837 cells with IC50s of 2.23 µM and 15.41 µM, respectively.
In Vivo

AP4-43 (1-100 µM; p.o.; continuous feeding in media) enhances survival of a patient-matched Drosophila colorectal cancer model by targeting a multi-kinase network including CLK1 and NEK4, with synergistic efficacy observed when combined with reduced NEK4 gene dosage, reaching 78.5% survival in this context[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Drosophila melanogaster (using byn-GAL4, UAS-GFP, GAL80ts and UAS-RAP-p1 transgenic lines; transgenic model expressing oncogenic RasG12V plus shRNAs targeting orthologues of human tumour suppressors Apc, P53, ago, wts, CG7742, and Atg2 in larval hindgut)[1]
Dosage: 1 µM; 10 µM; 100 µM
Administration: p.o.; continuous feeding in media
Result: Significantly improved byn>RAP-p1 survival over parent compound AP2-83 across multiple concentrations.
Reached 16.83% survival in byn>RAP-p1 flies at 10 µM alone.
Increased byn>RAP-p1; nek4-/+ fly survival to 78.5% (P < 0.0001) and caused significant reduction in hindgut proliferation zone area when combined with heterozygous loss of Drosophila NEK4 orthologue at 10 µM.
Improved survival in byn>RAP-p1; dyrk3-/+ flies when combined with heterozygous loss of CLK1 orthologue at 10 µM.
Did not improve survival in byn>RAP-p1; ddr-/+ flies at 10 µM.
Reduced survival in byn>RAP-p1; egfr-/+ flies at 10 µM.
Molecular Weight

382.18

Formula

C16H11BrF3N3
SMILES

BrC1=CC2=C(NC3=CC=C(C)C(C(F)(F)F)=C3)N=CN=C2C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AP4-43 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AP4-43NEKsCDKDiscoidin Domain ReceptorEGFRPI3KNIMA–related KinasesNIMA (never in mitosis gene a)-related Expressed KinasesCyclin dependent kinaseEpidermal growth factor receptorErbB-1HER1Phosphoinositide 3-kinasetransgenic DrosophilaDDR1mammalian colorectal cancer organoidsCLK4NEK4CLK1SW837 cellsSW620 human KRAS-driven colorectal cancer cellsKRAS-mutant colorectal cancerInhibitorinhibitorinhibit

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