1. Protein Tyrosine Kinase/RTK
  2. c-Kit
  3. APcK110

APcK110 is a potent Kit inhibitor that can be used for the research of acute myeloid leukemia (AML). APcK110 induces AML cell apoptosis.

For research use only. We do not sell to patients.

APcK110 Chemical Structure

APcK110 Chemical Structure

CAS No. : 1001083-74-4

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Description

APcK110 is a potent Kit inhibitor that can be used for the research of acute myeloid leukemia (AML). APcK110 induces AML cell apoptosis[1].

In Vitro

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.

Cell Proliferation Assay[1]

Cell Line: OCI/AML3, HMC1.2, BaF3 and mutant KIT-expressing BaF3 cells
Concentration: 0-500 nM
Incubation Time: 0, 24, 48 and 72 h
Result: Inhibited proliferation in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: OCI/AML3 and HMC1.2
Concentration: 0, 50, 100, 250 and 500 nM
Incubation Time: 30 min
Result: Showed a dose-dependent inhibition of the phosphorylation of Kit, Stat3, Stat5, and Akt, a downstream effector of phosphatidylinositol 3-kinase.

Apoptosis Analysis[1]

Cell Line: OCI/AML3 cells
Concentration: 500 nM
Incubation Time: Overnight
Result: Induced apoptosis by activation of the caspase pathway.

Cell Cycle Analysis[1]

Cell Line: OCI/AML3 cells
Concentration: 500 nM
Incubation Time: 2 h
Result: Showed a shift of cells into sub-G0 following a 2 h incubation.
In Vivo

APcK110 (500 nM; i.p.; every other day for 60 days) shows anti-AML activity in mice[2].

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

Animal Model: Eight-weeks-old female NODSCID mice, OCI/AML3 xenograft mouse model[2]
Dosage: 500 nM
Administration: Intraperitoneal injection, every other day for 60 days
Result: Survival of compound-treated mice was significantly longer compared with mice injected with PBS.
Molecular Weight

349.36

Formula

C20H16FN3O2

CAS No.
SMILES

FC1=CC=C(C2=NNC3=NC(C4=CC(OC)=CC(OC)=C4)=CC=C23)C=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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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.

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Product Name:
APcK110
Cat. No.:
HY-110071
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