Sotrastaurin

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Molecular Weight:

438.48 Sotrastaurin is a potent and selective Pan-PKC Inhibitor, mostly for PKCθ with Ki of 0.22 nM; inactive to PKCζ. Phase 2.


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 2.
Targets	PKCθ [1]	PKCβ1 [1]	PKCα [1]	PKCη [1]	PKCδ [1]	PKCε [1]
IC50	0.22 nM(Ki)	0.64 nM(Ki)	0.95 nM(Ki)	1.8 nM(Ki)	2.1 nM(Ki)	3.2 nM(Ki)
In vitro	Sotrastaurin ([1] Sotrastaurin([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.
Features	Unlike former PKC Inhibitors, Sotrastaurin does not enhance Apoptosis of murine T-cell blasts in a model of activation-induced cell death.

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.

Animal Study: [3]

Animal Models	male Wistar/F rats
Formulation	Saline
Dosages	10 mg/kg and 30 mg/kg
Administration	Orally administrated

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-02-07)

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT02285244	Not yet recruiting	Prolymphocytic Leukemia|Recurrent Mantle Cell Lymphoma|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Richter Syndrome	James Blachly|Novartis|Ohio State University Comprehensiv ...more James Blachly|Novartis|Ohio State University Comprehensive Cancer Center	January 2015	Phase 2
NCT02285244	Not yet recruiting	Prolymphocytic Leukemia|Recurrent Mantle Cell Lymphoma|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Richter Syndrome	James Blachly|Novartis|Ohio State University Comprehensiv ...more James Blachly|Novartis|Ohio State University Comprehensive Cancer Center	January 2015	Phase 2
NCT02273219	Recruiting	Uveal Melanoma	Gary Schwartz|Columbia University	November 2014	Phase 1
NCT02273219	Recruiting	Uveal Melanoma	Gary Schwartz|Columbia University	November 2014	Phase 1
NCT01854606	Recruiting	CD79 Mutant or ABC-subtype Diffuse Large B-Cell Lymphoma	Novartis Pharmaceuticals|Novartis	December 2013	Phase 1|Phase 2

Chemical Information

Molecular Weight (MW)	438.48
Formula	C25H22N6O2
CAS No.	425637-18-9

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	AEB071

Solubility (25°C) *	In vitro	DMSO	87 mg/mL (198.41 mM)
		Water	<1 mg/mL (
		Ethanol	2 mg/mL (4.56 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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Research Area




Product Citations (2)




Heat shock protein 90 controls HIV-1 reactivation from latency. [Anderson I, et al. Proc Natl Acad Sci U S A 2014;111(15):E1528-37]




PubMed: 24706778






ICAM-1-mediated leukocyte adhesion is critical for the activation of endothelial LSP1. [Hossain M, et al. Am J Physiol Cell Physiol 2013;304(9):C895-904]




PubMed: 23447036











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Tech Support & FAQs




Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store Inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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