WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H591244
CAS#: 908351-31-5 (acetate)
Description: Sotrastaurin, also known as AEB-071, is an orally available pan-protein kinase C (PKC) inhibitor with potential immunosuppressive and antineoplastic activities. Sotrastaurin inhibits both T- and B-cell activations via PKC theta and beta isozymes, respectively. Both PKCs are important in the activation of nuclear factor-kappaB (NF-kB). Inhibition of PKC beta in B-cells results in prevention of NF-kB-mediated signaling and down regulation of NF-kB target genes. This may eventually lead to an induction of G1 cell cycle arrest and tumor cell apoptosis in susceptible tumor cells. This agent may act synergistically with other chemotherapeutic agents.
Hodoodo Cat#: H591244
Name: Sotrastaurin acetate
CAS#: 908351-31-5 (acetate)
Chemical Formula: C27H26N6O4
Exact Mass: 498.20
Molecular Weight: 498.540
Elemental Analysis: C, 65.05; H, 5.26; N, 16.86; O, 12.84
This product is not in stock, which may be available by custom synthesis.
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Related CAS #: 908351-31-5 (acetate) 425637-18-9 (free base)
Synonym: Sotrastaurin acetate; AEB071; AEB071; AEB 071; Sotrastaurin;
IUPAC/Chemical Name: 1H-Pyrrole-2,5-dione, 3-(1H-indol-3-yl)-4-(2-(4-methyl-1-piperazinyl)-4-quinazolinyl)-, acetate
InChi Key: RVEUYBMXVVDLFO-UHFFFAOYSA-N
InChi Code: InChI=1S/C25H22N6O2.C2H4O2/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;1-2(3)4/h2-9,14,26H,10-13H2,1H3,(H,29,32,33);1H3,(H,3,4)
SMILES Code: O=C(C(C1=CNC2=C1C=CC=C2)=C3C4=C5C=CC=CC5=NC(N6CCN(C)CC6)=N4)NC3=O.CC(O)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
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The following data is based on the product molecular weight 498.54 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Wallner FK, Hultquist Hopkins M, Woodworth N, Lindvall Bark T, Olofsson P, Tilevik A. Correlation and cluster analysis of immunomodulatory drugs based on cytokine profiles. Pharmacol Res. 2018 Feb;128:244-251. doi: 10.1016/j.phrs.2017.10.012. Epub 2017 Oct 25. PubMed PMID: 29079427.
2: Zheng J, Kong C, Yang X, Cui X, Lin X, Zhang Z. Protein kinase C-α (PKCα) modulates cell apoptosis by stimulating nuclear translocation of NF-kappa-B p65 in urothelial cell carcinoma of the bladder. BMC Cancer. 2017 Jun 19;17(1):432. doi: 10.1186/s12885-017-3401-7. PubMed PMID: 28629334; PubMed Central PMCID: PMC5477139.
3: El-Gamal D, Williams K, LaFollette TD, Cannon M, Blachly JS, Zhong Y, Woyach JA, Williams E, Awan FT, Jones J, Andritsos L, Maddocks K, Wu CH, Chen CS, Lehman A, Zhang X, Lapalombella R, Byrd JC. PKC-β as a therapeutic target in CLL: PKC inhibitor AEB071 demonstrates preclinical activity in CLL. Blood. 2014 Aug 28;124(9):1481-91. doi: 10.1182/blood-2014-05-574830. Epub 2014 Jul 7. PubMed PMID: 25001469; PubMed Central PMCID: PMC4148770.
4: Capsoni F, Ongari AM, Reali E, Bosè F, Altomare GF. The protein kinase C inhibitor AEB071 (sotrastaurin) modulates migration and superoxide anion production by human neutrophils in vitro. Int J Immunopathol Pharmacol. 2012 Jul-Sep;25(3):617-26. PubMed PMID: 23058012.
5: Jakab A, Winter S, Guy B, Raccuglia M, Picard F, Kovarik JM, Chudasama J, Guttikar S, Singhal P, Kretz O. Validation of a liquid chromatography/tandem mass spectrometry method for the simultaneous quantification of Sotrastaurin and its metabolite N-desmethyl-sotrastaurin in human blood. J Chromatogr B Analyt Technol Biomed Life Sci. 2012 May 15;897:10-6. doi: 10.1016/j.jchromb.2012.03.039. Epub 2012 Apr 2. PubMed PMID: 22541169.
6: Matz M, Weber U, Mashreghi MF, Lorkowski C, Ladhoff J, Kramer S, Neumayer HH, Budde K. Effects of the new immunosuppressive agent AEB071 on human immune cells. Nephrol Dial Transplant. 2010 Jul;25(7):2159-67. doi: 10.1093/ndt/gfp775. Epub 2010 Jan 25. PubMed PMID: 20100729.
7: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2008 Apr;30(3):231-51. PubMed PMID: 18597009.
