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

Description Application

Product Name: 3-(1H-Indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione
CAS No.: 425637-18-9
Chemical Name: 3-(1H-Indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione
Synonyms: CS-1479;Dusquetide;Sotrastaurin;Sotrastaurin (AEB071);Glycerol Impurity 111;AEB071; AEB 071; AEB-071;1H-benzo[d][1,2,3]triazol-5-ol;Sotrastaurin - AEB 071 | NVP-AEB 071;3-(1H-Indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione;3-(1H-indol-3-yl)-4-(2-(4-methylpiperazin-1-yl)quinazolin-4-yl)-1H-pyrrole-2,5-dione
CBNumber: CB92510056
Molecular Formula: C25H22N6O2
Formula Weight: 438.48
MOL File: 425637-18-9.mol

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

Density: 1.406
storage temp.: Store at -20°C
solubility: ≥21.9 mg/mL in DMSO; insoluble in H2O; ≥2.55 mg/mL in EtOH with ultrasonic
form: solid
pka: 7.39±0.60(Predicted)
color: Pink to red

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H317May cause an allergic skin reaction

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML3210
Product name: Sotrastaurin
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $86.8
Updated: 2023/06/20

Sigma-Aldrich

Product number: SML3210
Product name: Sotrastaurin
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $280
Updated: 2023/06/20

Cayman Chemical

Product number: 16726
Product name: Sotrastaurin
Purity: ≥98%
Packaging: 1mg
Price: $49
Updated: 2024/03/01

Cayman Chemical

Product number: 16726
Product name: Sotrastaurin
Purity: ≥98%
Packaging: 5mg
Price: $202
Updated: 2024/03/01

Cayman Chemical

Product number: 16726
Product name: Sotrastaurin
Purity: ≥98%
Packaging: 10mg
Price: $356
Updated: 2024/03/01

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3-(1H-Indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione Chemical Properties,Usage,Production

Description

Sotrastaurin (AEB071) is a potent and selective pan-PKC inhibitor, most potent against PKCθ with Ki of 0.22 nM in a cell-free assay; no activity against PKCζ.

Application

Sotrastaurin has been used in trials studying the basic science and treatment of Uveal Melanoma, Richter Syndrome, Prolymphocytic Leukemia, Recurrent Mantle Cell Lymphoma, and Recurrent Small Lymphocytic Lymphoma, among others.

Uses

A potent selective pan-PKC inhibitor and highly inhibits PKCθ with a Ki of 0.22 nM.

Uses

Sotrastaurin is an protein kinase C inhibitor that modulates migration and superoxide anion production by human neutrophils in vitro.

Definition

ChEBI: A member of the class of maleimides that is maleimide which is substituted at position 3 by an indol-3-yl group and at position 4 by a quinazolin-4-yl group, which in turn is substituted at position 2 by a 4-methylpiperazin-1-yl group. It is a potent and s lective inhibitor of protein kinase C and has been investigated as an immunosuppresant in renal transplant patients.

Biological Activity

aeb071 is an inhibitor of protein kinase c (pkc). the pkc inhibitor which can block the t-cell activation has the ability of immune suppression [1].the protein kinase c (pkc) isoforms is very important in cell signaling, proliferation, differentiation, migration, survival, and death. pkc family has many isoforms. among the pkc isoforms, pkc isoforms have basal effect on the t cells’ activation and other immune cell functions [2,3].abe071 is a potent inhibitor of novel and classical pkc isoforms. through the inhibition of pkc, aeb071 can depress the activation and proliferation of t-cell and decrease the production of cytokine.abe071 can also suppress the nk cell activity. ex vivo stimulation of lymphocytes from subjects exposed to single doses of aeb071 resulted in a dose-dependent inhibition of both lymphocyte proliferation and il2 mrna expressionaeb071 is an effective treatment strategy for the cure of autoimmune diseases. according to the psoriasis area severity index (pasi) score, after 2 weeks’ treatment with 300 mg bid aeb071, clinical severity of psoriasis was reduced up to 69% compared with baseline[2,3].

References

[1]. weckbecker g1, pally c, beerli c, et al. effects of the novel protein kinase c inhibitor aeb071 (sotrastaurin) on rat cardiac allograft survival using single agent treatment or combination therapy with cyclosporine, everolimus or fty720. transpl int. 2010 may 1;23(5):543-52
[2]. skvara h1, dawid m, kleyn e, wolff b, et al. the pkc inhibitor aeb071 may be a therapeutic option for psoriasis. j clin invest. 2008 sep;118(9):3151-9.
[3]. matz m1, weber u, mashreghi mf, et al. effects of the new immunosuppressive agent aeb071 on human immune cells. nephrol dial transplant. 2010 jul;25(7):2159-67

3-(1H-Indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione Preparation Products And Raw materials

Raw materials

Preparation Products

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

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425637-18-9, 3-(1H-Indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dioneRelated Search:

Indole 5-Methoxy-alpha-methyltryptamine Enzastaurin (LY317615) GO 6983 MK-2206 2HCl Erlotinib hydrochloride PD 0332991 HCl Ibrutinib

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

Sotrastaurin

Sotrastaurin (AEB071)

3-(1H-indol-3-yl)-4-(2-(4-methylpiperazin-1-yl)quinazolin-4-yl)-1H-pyrrole-2,5-dione

Dusquetide

Sotrastaurin - AEB 071 | NVP-AEB 071

CS-1479

AEB071; AEB 071; AEB-071

1H-benzo[d][1,2,3]triazol-5-ol

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-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione USP/EP/BP

Glycerol Impurity 111

425637-18-9

Smad

TGF-beta

Inhibitors