AP4-43
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 99.76%
- Formula: C16H11BrF3N3
- Molecular Weight:382.18
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
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CLK1 |
CLK4 |
NEK4 |
DDR1 |
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.
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Cell Line:SW620 and SW837 cell lines
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Concentration:10 pM; 100 pM; 1 nM; 10 nM; 100 nM; 1 μM; 10 μM; 100 μM
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Incubation Time:72 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:1 µM; 10 µM; 100 µM
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Administration:p.o.; continuous feeding in media
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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
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Appearance Solid
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Molecular Weight 382.18
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Formula C16H11BrF3N3
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SMILES
BrC1=CC2=C(NC3=CC=C(C)C(C(F)(F)F)=C3)N=CN=C2C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AP4-43 Related Classifications
HY-183068 Related Classifications
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