Structure via PubChem · Public domain (PubChem)
enzastaurin
Sign in to saveAlso known as LY-317615, LY317615
Enzastaurin is a synthetic bisindolylmaleimide with potential antineoplastic activity. Binding to the ATP-binding site, enzastaurin selectively inhibits protein kinase C beta, an enzyme involved in the induction of vascular endothelial growth factor (VEGF)-stimulated neo-angiogenesis. This agent may decrease tumor blood supply, preventing growth.
Chemical data
- Formula
- C32H29N5O2
- Molecular weight
- 515.6 g/mol
- IUPAC name
- 3-(1-methylindol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]indol-3-yl]pyrrole-2,5-dione
- 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
- InChIKey
- AXRCEOKUDYDWLF-UHFFFAOYSA-N
- XLogP
- 3.7
- Polar surface area
- 72.2 Ų
- H-bond donors
- 1
- H-bond acceptors
- 4
- Formal charge
- 0
via PubChem
Drug data · ChEMBL
- Max clinical phase
- Phase 3
- Molecule type
- Small molecule
- Indications
- Mantle cell lymphoma, lymphoma, glioblastoma multiforme, neoplasm of mature B-cells
via ChEMBL · EBI
Wikidata facts
- Subclass of
- chemical compound
- Has part
- carbon
- Mass
- 515.232
- Has use
- medication
Show 3 more facts
- Commons category
- Enzastaurin
- chemical formula
- C₃₂H₂₉N₅O₂
- 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
Sources (2)
via Wikidata · CC0
~1 min read
Encyclopedic overview
3 sectionsContents
- Trials
- References
- External links
{{chembox | Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 443978959 | ImageFile = Enzastaurin.png | ImageSize = 180px | PIN = 3-(1-Methyl-1H-indol-3-yl)-4-(1-{1-[(pyridin-2-yl)methyl]piperidin-4-yl}-1H-indol-3-yl)-1H-pyrrole-2,5-dione | OtherNames = LY-317615 |Section1= |Section2= |Section3= }}
Enzastaurin is a synthetic bisindolylmaleimide with potential antineoplastic activity. Binding to the ATP-binding site, enzastaurin selectively inhibits protein kinase C beta, an enzyme involved in the induction of vascular endothelial growth factor (VEGF)-stimulated neo-angiogenesis. This agent may decrease tumor blood supply, preventing growth.
Excerpted from Wikipedia’s “enzastaurin” article, available under the CC BY-SA 4.0 licence.