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425637-18-9-Sotrastaurin Sotrastaurin

Sotrastaurin

For research use only. Not for therapeutic Use.

  • CAT Number: I003527
  • CAS Number: 425637-18-9
  • Molecular Formula: C25H22N6O2
  • Molecular Weight: 438.5
  • Purity: ≥95%
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Related products: Terpinyl Acetate     Demethyleneberberine     Efetaal    
Research Areas: Cytokine and Chemokine     Inflammation&Immunology Research    

Sotrastaurin (Cat.No:I003527), a first-in-class protein kinase C (PKC) inhibitor, is aiming to become the first oral treatment that inhibits T-cell activation since the introduction of calcineurin inhibitors. T-cell activation is an early step in autoimmune diseases such as psoriasis and is also essential for the rejection of transplanted organs. Sotrastaurin blocks a pathway critical to T-cell activation and has shown promise in organ transplantation as well as in autoimmune disorders. Sotrastaurin is developed for the potential treatment of psoriatic skin lesions and graft rejection.


Catalog Number I003527
CAS Number 425637-18-9
Synonyms

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

Molecular Formula C25H22N6O2
Purity ≥95%
Target PKC
Solubility in DMSO > 10 mM
Storage 3 years -20℃ powder
IUPAC Name 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione
InChI InChI=1S/C25H22N6O2/c1-30-10-12-31(13-11-30)25-27-19-9-5-3-7-16(19)22(28-25)21-20(23(32)29-24(21)33)17-14-26-18-8-4-2-6-15(17)18/h2-9,14,26H,10-13H2,1H3,(H,29,32,33)
InChIKey OAVGBZOFDPFGPJ-UHFFFAOYSA-N
SMILES CN(CC1)CCN1C2=NC3=CC=CC=C3C(C(C(N4)=O)=C(C5=CNC6=C5C=CC=C6)C4=O)=N2
Reference

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1:Inhibition of JAK3 and PKC via Immunosuppressive Drugs Tofacitinib and Sotrastaurin Inhibits Proliferation of Human B Lymphocytes In&nbsp;Vitro. Martina MN, Ramirez Bajo MJ, Ba&#241;on-Maneus E, Moya Rull D, Hierro-Garcia N, Revuelta I, Campistol JM, Rovira J, Diekmann F.Transplant Proc. 2016 Nov;48(9):3046-3052. doi: 10.1016/j.transproceed.2016.07.052. PMID: 27932144 <br />
2:Efficacy and Safety of Elective Conversion From Sotrastaurin (STN) to Tacrolimus (TAC) or Mycophenolate (MPS) in Stable Kidney Transplant Recipients. Hannun P, Felipe C, Ferreira A, Sandes-Freitas T, Cristelli M, Aguiar W, Franco M, Campos E, Gerbase de Lima M, Tedesco-Silva H, Medina-Pestana J.Ther Drug Monit. 2016 Jun;38(3):293-9. doi: 10.1097/FTD.0000000000000292. PMID: 26919549 <br />
3:Sotrastaurin in liver transplantation: has it had a fair trial? Trotter JF, Levy G.Am J Transplant. 2015 May;15(5):1137-8. doi: 10.1111/ajt.13179. Epub 2015 Feb 12. No abstract available. PMID: 25677186 Free Article<br />
4:Protein kinase C inhibitor sotrastaurin in de novo liver transplant recipients: a randomized phase II trial. Pascher A, De Simone P, Pratschke J, Salamé E, Pirenne J, Isoneimi H, Bijarnia M, Krishnan I, Klupp J.Am J Transplant. 2015 May;15(5):1283-92. doi: 10.1111/ajt.13175. Epub 2015 Feb 12. PMID: 25677074 Free Article<br />
5:Docetaxel Facilitates Endothelial Dysfunction through Oxidative Stress via Modulation of Protein Kinase C Beta: The Protective Effects of Sotrastaurin. Hung CH, Chan SH, Chu PM, Tsai KL.Toxicol Sci. 2015 May;145(1):59-67. doi: 10.1093/toxsci/kfv017. Epub 2015 Jan 28. PMID: 25634538 Free PMC Article<br />
6:Targeting PKC in human T cells using sotrastaurin (AEB071) preserves regulatory T cells and prevents IL-17 production. He X, Koenen HJ, Smeets RL, Keijsers R, van Rijssen E, Koerber A, van de Kerkhof PC, Boots AM, Joosten I.J Invest Dermatol. 2014 Apr;134(4):975-83. doi: 10.1038/jid.2013.459. Epub 2013 Nov 5. PMID: 24192715 Free Article<br />
7:The protein kinase C inhibitor sotrastaurin allows regulatory T cell function. de Weerd A, Kho M, Kraaijeveld R, Zuiderwijk J, Weimar W, Baan C.Clin Exp Immunol. 2014 Feb;175(2):296-304. doi: 10.1111/cei.12225. PMID: 24131367 Free PMC Article<br />
8:Efficacy of sotrastaurin plus tacrolimus after de novo kidney transplantation: randomized, phase II trial results. Russ GR, Tedesco-Silva H, Kuypers DR, Cohney S, Langer RM, Witzke O, Eris J, Sommerer C, von Zur-Mühlen B, Woodle ES, Gill J, Ng J, Klupp J, Chodoff L, Budde K.Am J Transplant. 2013 Jul;13(7):1746-56. doi: 10.1111/ajt.12251. Epub 2013 May 13. PMID: 23668931 Free Article<br />
9:Sotrastaurin in calcineurin inhibitor-free regimen using everolimus in de novo kidney transplant recipients. Tedesco-Silva H, Kho MM, Hartmann A, Vitko S, Russ G, Rostaing L, Budde K, Campistol JM, Eris J, Krishnan I, Gopalakrishnan U, Klupp J.Am J Transplant. 2013 Jul;13(7):1757-68. doi: 10.1111/ajt.12255. Epub 2013 May 9. PMID: 23659755 Free Article<br />
10:The protein kinase C inhibitor AEB071 (sotrastaurin) modulates migration and superoxide anion production by human neutrophils in vitro. Capsoni F, Ongari AM, Reali E, Bosè F, Altomare GF.Int J Immunopathol Pharmacol. 2012 Jul-Sep;25(3):617-26. PMID: 23058012

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