PI3Kδ-IN-24
PI3Kδ-IN-24 is a selective PI3Kδ inhibitor (IC50 = 0.1 nM). PI3Kδ-IN-24 exhibits significant antiproliferative effects against PI3Kδ-overexpressing cancer cell lines. PI3Kδ-IN-24 reduces p-AKT levels and induces cell cycle arrest and apoptosis in tumor cells. PI3Kδ-IN-24 is useful in cancer research, such as diffuse large B-cell lymphoma (DLBCL).
For research use only. We do not sell to patients.
- CAS No.: 3051829-20-7
- Formula: C28H29N7O4
- Molecular Weight:527.57
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
PI3Kδ 0.1 nM (IC50) |
PI3Kγ 1.97 nM (IC50) |
PI3Kα 97.85 nM (IC50) |
PI3Kδ-IN-24 (Compound M7) (72 h) inhibits cell growth against SU-DHL-6 and Pfeiffer cells, with GI50s of 0.012 μM and 0.068 μM, and exhibits weak antiproliferative activity against HCT-116, MCF-7 and Raji cells, with GI50s of 1.20 μM, 2.56 μM, 6.83 μM[1].
PI3Kδ-IN-24 (10-1000 nM, 24 h) continuously inhibits AKT phosphorylation in SU-DHL-6 cells[1].
PI3Kδ-IN-24 (10 μM, 0.5 h) increases the thermal stability of endogenous PI3Kδ in SU-DHL-6 cells[1].
PI3Kδ-IN-24 (0.01-1 μM, 24-72 h) arrests the growth in the G0/G1 phase and triggers apoptosis in SU-DHL-6 cells, but does not induce apoptosis in HEK293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:SU-DHL-6 cells
-
Concentration:10 nM, 33 nM, 100 nM, 333 nM, 1000 nM
-
Incubation Time:24 h
-
Result:Reduced the expression level of p-AKT.
-
Cell Line:SU-DHL-6 cells
-
Concentration:0.01 μM, 0.1 μM, 1 μM
-
Incubation Time:24 h
-
Result:Arrested the growth in the G0/G1 phase, blocked over 50 % in this phase at 0.1 μM, surpassing the efficacy of Idelalisib (HY-13026) at 10 μM.
-
Cell Line:SU-DHL-6 cells
-
Concentration:0.01 μM, 0.1 μM, 1 μM
-
Incubation Time:72 h
-
Result:Triggered apoptosis, induced apoptosis in approximately 60 % at 1 μM, surpassed Idelalisib in its capacity to promote apoptosis.
Chemical Information
-
CAS No. 3051829-20-7
-
Molecular Weight 527.57
-
Formula C28H29N7O4
-
SMILES
COC1=C(C=C(C2=CC=C3N=CN=C(C3=N2)N[C@@H](C)C(N4CCN(CC4)C)=O)C=N1)C(OC5=CC=CC=C5)=O
-
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Powered by Bioz