- 貨號 Cat. No.
- S2791
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
Sotrastaurin
Sotrastaurin is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM; inactive to PKCζ. Phase 1/2.
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10mM/1mLIn DMSO |
USD 239 |
In stock |
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5mg |
USD 214 |
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25mg |
USD 844 |
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
Description |
Sotrastaurin is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM; inactive to PKCζ. Phase 1/2. |
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Targets |
PKCα |
PKCβ |
PKCδ |
PKCε |
PKCη |
PKCθ |
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IC50 |
0.95 nM (Ki) |
0.64 nM (Ki) |
2.1 nM (Ki) |
3.2 nM (Ki) |
1.8 nM (Ki) |
0.22 nM (Ki) [1] |
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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] |
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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] |
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Features |
Unlike former PKC inhibitors, Sotrastaurin does not enhance apoptosis of murine T-cell blasts in a model of activation-induced cell death. |
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Protocol(Only for Reference)
Kinase Assay: [1]
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. |
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Animal Study: [3]
Animal Models |
male Wistar/F rats |
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Dosages |
10 mg/kg and 30 mg/kg |
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Administration |
Orally administrated |
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1
References
Clinical Trial Information( data from http://clinicaltrials.gov)
NCT Number |
Recruitment |
Conditions |
Sponsor
/Collaborators |
Start Date |
Phases |
|---|
NCT01128335 |
Completed |
Liver Transplantation |
Novartis|Novartis Pharmaceuticals |
2010-04 |
Phase 2 |
NCT01402440 |
Recruiting |
Diffuse Large B-Cell Lymphoma |
Novartis|Novartis Pharmaceuticals |
2011-11 |
Phase 1 |
NCT01430416 |
Recruiting |
Uveal Melanoma |
Novartis|Novartis Pharmaceuticals |
2011-12 |
Phase 1 |
NCT01801358 |
Not yet recruiting |
Uveal Melanoma |
Novartis|Novartis Pharmaceuticals |
2013-07 |
Phase 1|Phase 2 |
NCT01854606 |
Not yet recruiting |
CD79 Mutant or ABC-subtype Diffuse Large B-Cell Lymphoma |
Novartis|Novartis Pharmaceuticals |
2013-09 |
Phase 1|Phase 2 |
Download Sotrastaurin SDF
Molecular Weight (MW) |
438.48 |
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Formula |
C25H22N6O2
|
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CAS No. |
425637-18-9 |
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Storage |
3 years -20℃Powder |
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6 months-80℃in DMSO |
Syonnyms |
N/A |
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Solubility (25°C) * |
In vitro |
DMSO |
87 mg/mL (198 mM) |
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Water |
<1 mg/mL (<1 mM) |
Ethanol |
2 mg/mL (4 mM) |
* <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. |
Chemical Name |
3-(1H-indol-3-yl)-4-(2-(4-methylpiperazin-1-yl)quinazolin-4-yl)-1H-pyrrole-2,5-dione |
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Stock Solution (1ml DMSO) |
1mM |
10mM |
20mM |
30mM |
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Mass(mg) |
0.43848 |
4.3848 |
8.7696 |
13.1544 |
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