Cat. No.: HY-183068

AP4-43

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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.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté: 99.76%
Formule: C₁₆H₁₁BrF₃N₃
Masse moléculaire:382.18

Stockage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

AP4-43 Chemical Structure

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Top Publications Citing

Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

CLK1

CLK4

NEK4

DDR1

Voir tous les produits spécifiques à Isoform NEKs :

Voir tous les produits spécifiques à Isoform CDK :

Voir tous les produits spécifiques à Isoform Discoidin Domain Receptor :

DDR1
DDR2

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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.

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 Ras^G12V 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.

Chemical Information

Appearance Solid
Masse moléculaire 382.18
Formule C₁₆H₁₁BrF₃N₃
SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Badmos HA, et al. Chemical programming of kinase inhibitors in a modular chemputer-based system. Commun Biol. Published online March 27, 2026. [Content Brief]

Calculators

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Calculateur de dilution

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

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AP4-43

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Voir tous les produits spécifiques à Isoform NEKs

Voir tous les produits spécifiques à Isoform CDK

Voir tous les produits spécifiques à Isoform Discoidin Domain Receptor

Voir tous les produits spécifiques à Isoform EGFR

Voir tous les produits spécifiques à Isoform PI3K

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

AP4-43 Related Classifications

HY-183068 Related Classifications