2361418-65-5

2361418-65-5 structure
2361418-65-5 structure
  • Name: PI3K/HDAC-IN-2
  • Chemical Name: PI3K/HDAC-IN-2
  • CAS Number: 2361418-65-5
  • Molecular Formula: C23H23N7O4
  • Molecular Weight: 461.47
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage HDAC
  • Create Date: 2022-09-23 20:54:03
  • Modify Date: 2024-03-12 20:10:12
  • PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor with IC50s of 226 nM, 279 nM, 467 nM, 29 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively, and IC50s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM for HDAC1, HDAC2, HDC4, HDAC6, HDAC8, respectively. PI3K/HDAC-IN-2 exhibits PI3Kδ and class I and IIb HDAC selectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects[1].

Name PI3K/HDAC-IN-2
Description PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor with IC50s of 226 nM, 279 nM, 467 nM, 29 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively, and IC50s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM for HDAC1, HDAC2, HDC4, HDAC6, HDAC8, respectively. PI3K/HDAC-IN-2 exhibits PI3Kδ and class I and IIb HDAC selectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects[1].
Related Catalog
Target

PI3Kα:226 nM (IC50)

PI3Kβ:279 nM (IC50)

PI3Kγ:467 nM (IC50)

PI3Kδ:29 nM (IC50)

HDAC1:1.3 nM (IC50)

HDAC2:3.4 nM (IC50)

HDAC4:972 nM (IC50)

HDAC6:17 nM (IC50)

HDAC8:12 nM (IC50)

In Vitro For PI3K/HDAC-IN-2 (Compound 8), the IC50 values in the growth inhibition assay against MDA-MB-453, HCT116 and HGC-27 cells are as low as namomolar level, which are 4 nM, 7 nM and 14 nM respectively[1]. PI3K/HDAC-IN-2 (Compound 8) shows antiproliferative activities against 16 DLBCL cell lines with IC50s of 3.6-21 nM[1].
In Vivo In the zebrafish xenograft model of SU-DHL-4 cells, PI3K/HDAC-IN-2 (Compound 8) exhibits in vivo growth inhibitory activity at 3 μM[1].
References

[1]. Kehui Zhang, et al. Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. Bioorg Med Chem Lett. 2022 Sep 1;71:128825.

Molecular Formula C23H23N7O4
Molecular Weight 461.47