[CAS NO. 425637-18-9]  Sotrastaurin (AEB071)

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PRODUCTS SPECIFICATIONS [425637-18-9]

Store
Catalog
SLK-S2791
Brand
Selleck
CAS
425637-18-9

DESCRIPTION [425637-18-9]

Overview

MDLMFCD16038049
Molecular Weight438.48
Molecular FormulaC25H22N6O2
SMILESO=C1C(=C(C(=O)N1)C=2C=3C(NC2)=CC=CC3)C=4C5=C(N=C(N4)N6CCN(C)CC6)C=CC=C5

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.2806 mL11.4030 mL22.8061 mL
5 mM0.4561 mL2.2806 mL4.5612 mL
10 mM0.2281 mL1.1403 mL2.2806 mL
50 mM0.0456 mL0.2281 mL0.4561 mL

Description

Sotrastaurin (AEB071) is a potent and selective pan- inhibitor, mostly for with of 0.22 nM in a cell-free assay; inactive to PKCζ. Phase 2.

Features

Unlike former PKC inhibitors, Sotrastaurin does not enhance apoptosis of murine T-cell blasts in a model of activation-induced cell death.

Targets


In vitro

Sotrastaurin (< 10μM) treatment effectively abrogated at low nanomolar concentration markers of early T-cell activation, such as interleukin-2 secretion and CD25 expression, in primary human and mouse T cells. Sotrastaurin (200 nM) inhibits the CD3/CD28 antibody- and alloantigen-induced T-cell proliferation responses in the absence of nonspecific antiproliferative effects. Sotrastaurin (<3 μM) markedly inhibits lymphocyte function-associated antigen-1-mediated T-cell adhesion. Sotrastaurin(< 20 μM) selectively impair the proliferation of CD79 mutant ABC DLBCL cell lines, correlating with decreased NF-κB signaling avctivity. AEB071 at concentration of 5 μM induces G1 arrest and/or cell death in CD79 mutant cells.


Synonyms

1H-Pyrrole-2,5-dione, 3-(1H-indol-3-yl)-4-[2-(4-methyl-1-piperazinyl)-4-quinazolinyl]-
3-(1H-Indol-3-yl)-4-[2-(4-methyl-1-piperazinyl)-4-quinazolinyl]-1H-pyrrole-2,5-dione
Sotrastaurin
3-(1H-Indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione