APcK110
APcK110 is a potent Kit inhibitor that can be used for the research of acute myeloid leukemia (AML). APcK110 induces AML cell apoptosis.
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- CAS No.: 1001083-74-4
- Formule: C20H16FN3O2
- Masse moléculaire:349.36
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
APcK110 (0-500 nM; 0-72 h) inhibits AML cell viability and proliferation. APcK110 preferentially inhibits KIT mutated BaF3 cell lines[1].
APcK110 (0-500 nM; 30 min) inhibits the phosphorylation of Kit, Stat3, Stat5, and Akt[1].
APcK110 (500 nM; overnight) induces caspase-dependent apoptosis in OCI/AML3 cells[1].
APcK110 (50-500 nM; 7 days) inhibits AML blast colony-forming cell proliferation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:OCI/AML3, HMC1.2, BaF3 and mutant KIT-expressing BaF3 cells
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Concentration:0-500 nM
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Incubation Time:0, 24, 48 and 72 h
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Result:Inhibited proliferation in a dose-dependent manner.
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Cell Line:OCI/AML3 and HMC1.2
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Concentration:0, 50, 100, 250 and 500 nM
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Incubation Time:30 min
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Result:Showed a dose-dependent inhibition of the phosphorylation of Kit, Stat3, Stat5, and Akt, a downstream effector of phosphatidylinositol 3-kinase.
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Cell Line:OCI/AML3 cells
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Concentration:500 nM
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Incubation Time:Overnight
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Result:Induced apoptosis by activation of the caspase pathway.
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Cell Line:OCI/AML3 cells
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Concentration:500 nM
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Incubation Time:2 h
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Result:Showed a shift of cells into sub-G0 following a 2 h incubation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Eight-weeks-old female NODSCID mice, OCI/AML3 xenograft mouse model[2]
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Dosage:500 nM
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Administration:Intraperitoneal injection, every other day for 60 days
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Result:Survival of compound-treated mice was significantly longer compared with mice injected with PBS.
Chemical Information
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CAS No. 1001083-74-4
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Masse moléculaire 349.36
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Formule C20H16FN3O2
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SMILES
FC1=CC=C(C2=NNC3=NC(C4=CC(OC)=CC(OC)=C4)=CC=C23)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Faderl S, et al. Kit inhibitor APcK110 induces apoptosis and inhibits proliferation of acute myeloid leukemia cells. Cancer Res. 2009 May 1;69(9):3910-7. [Content Brief]
[2]. Faderl S, et al. Kit inhibitor APcK110 extends survival in an AML xenograft mouse model. Invest New Drugs. 2011 Oct;29(5):1094-7. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)