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{{chembox |
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{{chembox |
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| UNII_Ref = {{fdacite|correct|FDA}} |
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| UNII = UC96G28EQF |
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| verifiedrevid = 439320167 |
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| verifiedrevid = 443978959 |
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| ImageFile = Enzastaurin.png |
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| ImageFile = Enzastaurin.png |
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| ImageSize = 180px |
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| ImageSize = 180px |
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| IUPACName = 3-(1-Methylindol-3-yl)-4-]pyrrole-2,5-dione |
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| PIN = 3-(1-Methyl-1''H''-indol-3-yl)-4-(1-{1-piperidin-4-yl}-1''H''-indol-3-yl)-1''H''-pyrrole-2,5-dione |
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| OtherNames = LY-317615 |
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| OtherNames = LY-317615 |
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| Section1 = {{Chembox Identifiers |
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|Section1={{Chembox Identifiers |
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| UNII_Ref = {{fdacite|correct|FDA}} |
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| UNII = UC96G28EQF |
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| KEGG = D11935 |
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| IUPHAR_ligand = 5693 |
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| CASNo_Ref = {{cascite|correct|??}} |
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| CASNo = 170364-57-5 |
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| CASNo = 170364-57-5 |
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| PubChem = 176167 |
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| PubChem = 176167 |
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| ChEMBL_Ref = {{ebicite|changed|EBI}} |
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| 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 |
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| ChEMBL = 300138 |
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| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} |
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| ChemSpiderID = 153463 |
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| SMILES = O=C3C(\c2c1ccccc1n(c2)C)=C(/C(=O)N3)c5c4ccccc4n(c5)C7CCN(Cc6ncccc6)CC7 |
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| InChI = 1/C32H29N5O2/c1-35-19-25(23-9-2-4-11-27(23)35)29-30(32(39)34-31(29)38)26-20-37(28-12-5-3-10-24(26)28)22-13-16-36(17-14-22)18-21-8-6-7-15-33-21/h2-12,15,19-20,22H,13-14,16-18H2,1H3,(H,34,38,39) |
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| InChIKey = AXRCEOKUDYDWLF-UHFFFAOYAP |
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| StdInChI_Ref = {{stdinchicite|changed|chemspider}} |
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| StdInChI = 1S/C32H29N5O2/c1-35-19-25(23-9-2-4-11-27(23)35)29-30(32(39)34-31(29)38)26-20-37(28-12-5-3-10-24(26)28)22-13-16-36(17-14-22)18-21-8-6-7-15-33-21/h2-12,15,19-20,22H,13-14,16-18H2,1H3,(H,34,38,39) |
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| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} |
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| StdInChIKey = AXRCEOKUDYDWLF-UHFFFAOYSA-N |
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}} |
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| Section2 = {{Chembox Properties |
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|Section2={{Chembox Properties |
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| C=32|H=29|N=5|O=2 |
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| C=32 | H=29 | N=5 | O=2 |
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| Solubility = }} |
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| Solubility = }} |
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| Section3 = {{Chembox Hazards |
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|Section3={{Chembox Hazards |
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| MainHazards = |
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| FlashPt = |
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| Autoignition = }} |
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'''Enzastaurin''' is a synthetic ] with potential ] activity. Binding to the ATP-binding site, enzastaurin selectively inhibits ] beta, an enzyme involved in the induction of ] (VEGF)-stimulated neo-angiogenesis. This agent may decrease tumor blood supply, preventing growth. |
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'''Enzastaurin''' is a synthetic ] with potential ] activity. Binding to the ATP-binding site, enzastaurin selectively inhibits ] beta, an enzyme involved in the induction of ] (VEGF)-stimulated neo-angiogenesis. This agent may decrease tumor blood supply, preventing growth. |
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== Trials == |
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In 2013 it failed a phase III clinical trial for ].<ref name="GE2013"></ref> |
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In 2022, there is an upcoming initial trial called PREVEnt to look into the effectiveness of Enzastaurin for the treatment of ] (vEDS). <ref>{{Cite web|title=New vEDS clinical trial|url=https://preventvedstrial.com/|access-date=2022-01-19|website=PREVEnt Trial|language=en-US}}</ref><ref>{{Cite web|title=Aytu BioPharma Adds Late-Stage Pediatric Onset Rare Disease Asset to Development Pipeline from Rumpus Therapeutics|url=https://www.biospace.com/article/aytu-biopharma-adds-late-stage-pediatric-onset-rare-disease-asset-to-development-pipeline-from-rumpus-therapeutics/|access-date=2022-01-19|website=BioSpace|language=en-US}}</ref><ref>{{Cite web|title=Clinical Trials|url=https://www.fightveds.org/clinical-trials|access-date=2022-01-19|website=FIGHT vEDS 3.0|language=en}}</ref> |
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==References== |
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{{reflist}} |
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==External links== |
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==External links== |
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* , National Institutes of Health |
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* , National Institutes of Health |
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