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942289-87-4

942289-87-4 structure
942289-87-4 structure
  • Name: PI 828
  • Chemical Name: 8-(4-aminophenyl)-2-morpholin-4-ylchromen-4-one
  • CAS Number: 942289-87-4
  • Molecular Formula: C19H18N2O3
  • Molecular Weight: 322.35800
  • Catalog: Signaling Pathways PI3K/Akt/mTOR PI3K
  • Create Date: 2016-07-11 05:22:07
  • Modify Date: 2024-01-02 23:52:20
  • PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively[1].

Name 8-(4-aminophenyl)-2-morpholin-4-ylchromen-4-one
Synonyms HMS3229H13
W-84 dibromide
HMS3266C12
Description PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively[1].
Related Catalog
Target

p110α:173 nM (IC50)

CK2:149 nM (IC50)

CK2α2:1.127 μM (IC50)

In Vitro PI-828 (0.01-100 μM) exhibits cytotoxic effect on the 4T1 breast cancer cells and 4306 ovarian cancer cells[2]. PI-828 (0.78-3.12 µM; 48 hours) decreases caspase 3 activation; higher concentrations of PI-828 (6.25-12.5 μM) alone causes apoptosis[3]. Cell Viability Assay[2] Cell Line: 4T1 breast cancer cells and 4306 ovarian cancer cells Concentration: 0.01, 0.1, 1, 10 and 100 μM Incubation Time: Result: Exhibited cytotoxic effect. Apoptosis Analysis[3] Cell Line: Human embryonic carcinoma NCCIT cells Concentration: 0.78, 1.56, 3.12, 6.25, 12.5 μM Incubation Time: 48 hours Result: Concentrations of ranging from 0.78 to 3.12 µM decreased caspase 3 activation; higher concentrations caused apoptosis.
References

[1]. Gharbi SI, et al. Exploring the specificity of the PI3K family inhibitor LY294002. Biochem J. 2007 May 15;404(1):15-21.

[2]. Kulkarni AA, et al. Supramolecular nanoparticles that target phosphoinositide-3-kinase overcome insulin resistance and exert pronounced antitumor efficacy. Cancer Res. 2013 Dec 1;73(23):6987-97.

[3]. Zellefrow CD, et al. Identification of druggable targets for radiation mitigation using a small interfering RNA screening assay. Radiat Res. 2012 Sep;178(3):150-9.

Density 1.316g/cm3
Boiling Point 534.2ºC at 760 mmHg
Molecular Formula C19H18N2O3
Molecular Weight 322.35800
Flash Point 276.9ºC
Exact Mass 322.13200
PSA 68.70000
LogP 3.52500
Index of Refraction 1.658