Enzastaurin

Enzastaurin
Names
	IUPAC name 3-(1-Methylindol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]indol-3-yl]pyrrole-2,5-dione
	Other names LY-317615
Identifiers
CAS Number	170364-57-5 ;
3D model (JSmol)	Interactive image;
ChEMBL	ChEMBL300138 ;
ChemSpider	153463 ;
ECHA InfoCard	100.233.143
IUPHAR/BPS	5693;
PubChem CID	176167;
UNII	UC96G28EQF ;
CompTox Dashboard (EPA)	DTXSID5044029 ;
	InChI InChI=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) Key: AXRCEOKUDYDWLF-UHFFFAOYSA-N ; 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) Key: AXRCEOKUDYDWLF-UHFFFAOYAP;
	SMILES O=C3C(\c2c1ccccc1n(c2)C)=C(/C(=O)N3)c5c4ccccc4n(c5)C7CCN(Cc6ncccc6)CC7;
Properties
Chemical formula	C32H29N5O2
Molar mass	515.617 g·mol−1
	Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). verify (what is ?) Infobox references

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.

In 2013 it failed a phase III clinical trial for lymphoma.^[1]

References

^ Lilly Halts Development of Lymphoma Drug After Phase III Failure

External links

Enzastaurin hydrochloride, National Institutes of Health

[GE2013-1] Lilly Halts Development of Lymphoma Drug After Phase III Failure

[1]