Chemical Property of Enzastaurin
Chemical Property:
- Vapor Pressure:1.87E-23mmHg at 25°C
- Melting Point:249-261℃
- Refractive Index:1.722
- Boiling Point:767.2 °C at 760 mmHg
- PKA:7.88±0.60(Predicted)
- Flash Point:417.8 °C
- PSA：72.16000
- Density:1.34 g/cm3
- LogP:5.19900
- Storage Temp.:?20°C
- Solubility.:DMSO: soluble10mg/mL, clear (warmed)
- XLogP3:3.7
- Hydrogen Bond Donor Count:1
- Hydrogen Bond Acceptor Count:4
- Rotatable Bond Count:5
- Exact Mass:515.23212518
- Heavy Atom Count:39
- Complexity:974
- Purity/Quality:
-
99%, *data from raw suppliers
Enzastaurin *data from reagent suppliers
Safty Information:
- Pictogram(s):
Xn
- Hazard Codes:Xn
- Statements:
22
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CN(C5=CC=CC=C54)C6CCN(CC6)CC7=CC=CC=N7
- Recent ClinicalTrials:Investigate Efficacy, Safety, and Pharmacokinetics of Enzastaurin for the Prevention of Arterial Events in Patients With Vascular Ehlers-Danlos Syndrome.
- Recent EU Clinical Trials:A multicenter, randomized, double-blind, placebo-controlled study of enzastaurin for the prevention of arterial events in patients with vascular Ehlers-Danlos Syndrome (vEDS) confirmed with COL3A1 mutations, followed by an open label extension (OLE)
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Description
Enzastaurin (170364-57-5) is a potent and selective PKCβ inhibitor.? IC50 = 6, 39, 83 and 110 nM, for PKCβ, PKCα, PKCγ and PKCε respectively.1 Induces apoptosis in multiple myeloma cell lines via inhibition of the AKT signaling pathway.2 Induces mitotic missegregation and preferential cytotoxicity in colorectal cancer cells with chromosomal instability.3 Attenuates amphetamine-stimulated dopamine efflux.4 Inhibits blood-brain barrier leakiness in a mouse model.5
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Uses
PKCβ-selective inhibitor, suppresses angiogenesis. Enzastaurin has been used in splicing analysis to study its effects on splicing of a mutated exon.
