PI3K-IN-34

Names

[ CAS No. ]:
2458163-94-3

[ Name ]:
PI3K-IN-34

Biological Activity

[Description]:

PI3K-IN-34 (Compound 6g) is a highly selective PI3K inhibitor with IC50 values of 11.73, 6.09 and 11.18 μM for PI3K-α、PI3K-β and PI3K-δ , respectively. PI3K-IN-34 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-34 can be used in leukemia research[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> PI3K/Akt/mTOR >> PI3K

[Target]

PI3Kα:8.43 μM (IC50)

PI3Kβ:15.84 μM (IC50)

PI3Kδ:30.62 μM (IC50)


[In Vitro]

PI3K-IN-34 (Compound 6g) (10 μM, 48 hours) possess potent antiproliferative activity can inhibit proliferation of Leukemia SR cell lines in vitro[1]. PI3K-IN-34 (Compound 6g) induces cell cycle arrest toward the G2-M phase (45.75%) and leads to DNA synthesis and apoptosis[1]. PI3K-IN-34 (Compound 6g) (10 μM, 48 hours) results in apoptotic with 22.83% of cells in the early and latest age[1]. Cell Cytotoxicity Assay[1] Cell Line: Leukemia SR cell lines. Concentration: 10 μM Incubation Time: 48 hours Result: Antiproliferative activity with values of 4.37 μM.

[References]

[1]. Helwa AA, et al. Novel antiproliferative agents bearing morpholinopyrimidine scaffold as PI3K inhibitors and apoptosis inducers; design, synthesis and molecular docking. Bioorg Chem. 2020 Sep;102:104051.

Chemical & Physical Properties

[ Molecular Formula ]:
C23H22N6O3

[ Molecular Weight ]:
430.46


Related Compounds