Sotrastaurin (AEB071)

製品コードS2791 バッチS279101

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H22N6O2
分子量 438.48 CAS No. 425637-18-9
Solubility (25°C)* 体外 DMSO 87 mg/mL (198.41 mM)
Ethanol 2 mg/mL (4.56 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Sotrastaurin (AEB071) is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM in a cell-free assay; inactive to PKCζ. Phase 2.
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. [1]

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. [2]
in vivo

Sotrastaurin (80 mg/kg) results in significant inhibition of in vivo tumor growth in a subcutaneous TMD8 xenograft model in SCID. [2]

Sotrastaurin orally administrated at 10 mg/kg and 30 mg/kg b.i.d. show a dose-dependent immunosuppressive effect leading to pronounced prolongation of heart allograft survival in rats. [3]
特徴 Unlike former PKC inhibitors, Sotrastaurin does not enhance apoptosis of murine T-cell blasts in a model of activation-induced cell death.

プロトコル(参考用のみ)

キナーゼアッセイ Protein Kinase Assays
Classical and novel PKC isotypes are assayed by scintillation proximity assay technology. In brief, the assay is performed in 20 mM Tris-HCl buffer, pH 7.4, and 0.1% bovine serum albumin by incubating 1.5 μM of the peptide substrate with 10 μM [33P]ATP, 10 mM Mg (NO3)2, 0.2 mM CaCl2, and PKC at a protein concentration varying from 25 to 400 ng/mL, and lipid vesicles containing 30 mol% phosphatidylserine, 5 mol% diacylglycerol (DAG), and 65 mol% phosphatidylcholine at a final lipid concentration of 0.5 μM. Incubation is performed for 60 min at room temperature. The reaction is stopped by adding 50 μl of a mixture containing 100 mM EDTA, 200 μM ATP, 0.1% Triton X-100, and 0.375 μg/well streptavidin-coated scintillation proximity assay beads in PBS without Ca2+ and Mg2+. Incorporated radioactivity is measured in a MicroBetaTrilux counter for 1 min.
細胞アッセイ 細胞株 UM cell lines
濃度 5 μM
反応時間 24 h
実験の流れ

Cells were treated with indicated concentration of drug for 24 h.
動物実験 動物モデル male Wistar/F rats
投薬量 10 mg/kg and 30 mg/kg
投与方法 Orally administrated

カスタマーフィードバック

Data from [Data independently produced by , , Cancer Cell, 2015, 27(3): 397-408 ]

Data from [Data independently produced by , , Proc Natl Acad Sci USA, 2014, 111(15): E1528-37]

Data from [Data independently produced by , , Br J Haematol, 2016, 173(3):394-403]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Translational genetics identifies a phosphorylation switch in CARD9 required for innate inflammatory responses [ Cell Rep, 2024, 43(3):113944] PubMed: 38489265
Bactericidal/permeability-increasing protein instructs dendritic cells to elicit Th22 cell response [ Cell Rep, 2024, 43(3):113929] PubMed: 38457343
High-throughput chemogenetic drug screening reveals PKC-RhoA/PKN as a targetable signaling vulnerability in GNAQ-driven uveal melanoma [ Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101244] PubMed: 37858338
Alternative splicing of HDAC7 regulates its interaction with 14-3-3 proteins to alter histone marks and target gene expression [ Cell Rep, 2023, 42(3):112273] PubMed: 36933216
Alternative splicing of HDAC7 regulates its interaction with 14-3-3 proteins to alter histone marks and target gene expression [ Cell Rep, 2023, 42(3):112273] PubMed: 36933216
Trace amine-associated receptor 1 regulation of Kv1.4 channels in trigeminal ganglion neurons contributes to nociceptive behaviors [ J Headache Pain, 2023, 24(1):49] PubMed: 37158881
GATA1 deletion in human pluripotent stem cells increases differentiation yield and maturity of neutrophils [ iScience, 2023, 26(10):107804] PubMed: 37720099
Exercise-acclimated microbiota improves skeletal muscle metabolism via circulating bile acid deconjugation [ iScience, 2023, 26(3):106251] PubMed: 36915683
Exercise-acclimated microbiota improves skeletal muscle metabolism via circulating bile acid deconjugation [ iScience, 2023, 10.1016/j.isci.2023.106251] PubMed: 36915683
GATA1 deletion in human pluripotent stem cells increases differentiation yield and maturity of neutrophils [ iScience, 2023, 26(10):107804] PubMed: 37720099

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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