Sotrastaurin | PKC inhibitor

CAS:425637-18-9

Catalog Number:10-4350

Sotrastaurin (425637-18-9) is a highly selective and potent (IC50’s for PKC isotypes: α = 2.1 nM, ß1 = 2.0 nM, δ = 1.3 

nM, ε = 6.2 nM, η = 6.1 nM, Θ = 1.0 nM) pan-PKC inhibitor.1 Potent immunomodulatory agent that inhibits early T-cell 

activation and displays potential for the prevention of transplant rejection and the treatment of inflammatory diseases.

2,3 Sotrastaurin has anticancer activity in various cancer models including breast4, CLL5, ocular melanoma6, and 

B-cell lymphoma7.

425637-18-9, AEB-071, AEB071, pan-PKC inhibitor, PKC inhibitor, Sotrastaurin, Sotrastaurin supplier

CAS:425637-18-9

Catalog Number:10-4350

Activity:PKC inhibitor

Chemical Names:3-(1H-Indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione

Alternate Name:AEB071

Molecular Weight:438.49

Molecular Formula:C25H22N6O2

Solubility:Soluble in DMSO (>25 mg/ml)

Physical Properties:Orange solid

Purity:>98% HPLC

NMR: (Conforms)

Storage Temperature:-20°C

Stability:

Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.

Shipping Code:RT

References/Citations:

Wagner et al. (2009), Discovery of 3-(1H-Indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071),

a Potent and Selective Inhibitor of Protein Kinase C Isotypes; J. Med. Chem. 52 6193

Manicassamy (2009), Sotrastaurin, a protein kinase C inhibitor for the prevention of transplant rejection and treatment of 

psoriasis; Curr. Opin. Investig. Drugs 10 1225

Matz et al. (2011), Evaluation of the novel protein kinase C inhibitor sotrastaurin as immunosuppressive therapy after renal

transplantation; Expert Opin. Drug Metab. Toxicol. 7 103

Byerly et al. (2016), PRKCQ promotes oncogenic growth and anoikis resistance of a subset of triple-negative breast cancer cells; 

Breast Cancer Res. 18 95

El-Gamal et al. (2014), PKC-beta as a therapeutic target in CLL: PKC inhibitor AEB071 demonstrates preclinical activity in CLL; 

Blood 124 1481

Wu et al. (2012), Protein kinase C inhibitor AEB071 targets ocular melanoma harboring GNAQ mutations via effects on the PKC/Erk1/2

 and PKC/NF-kappaB pathways; Mol. Cancer Ther. 11 1905

Naylor et al. (2011), Protein kinase C inhibitor sotrastaurin selectively inhibits the growth of CD79 mutant diffuse large B-cell lymphomas; 

Cancer Res. 71 2643