Name | Enzastaurin |
Synonyms | Ly317615 Enzastaurin Enzastaurine Unii-uc96G28eqf Enzastaurin ( LY317615 ) Enzastaurin,Enzstataurin,LY317615,170364-57-5,1H-Pyrrole-2,5-dione, 3- 3-(1-Methyl-1H-indol-3-yl)-4-(1-(1-(2-pyridinylmethyl)-4-piperidinyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione 3-(1-methyl-1H-indol-3-yl)-4-{1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]-1H-indol-3-yl}-1H-pyrrole-2,5-dione 1H-Pyrrole-2,5-dione, 3-(1-methyl-1H-indol-3-yl)-4-(1-(1-(2-pyridinylmethyl)-4-piperidinyl)-1H-indol-3-yl)- |
CAS | 170364-57-5 |
InChI | 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) |
Molecular Formula | C32H29N5O2 |
Molar Mass | 515.6 |
Density | 1.34 |
Melting Point | 249-261℃ |
Boling Point | 767.2±60.0 °C(Predicted) |
Flash Point | 417.8℃ |
Solubility | Soluble in DMSO (30 mg/ml at 25 °C), water (< 1 mg/ml at 25 °C), ethanol (< 1 mg/m |
Vapor Presure | 1.87E-23mmHg at 25°C |
Appearance | powder |
Color | , light orange to dark orange-red |
pKa | 7.88±0.60(Predicted) |
Storage Condition | -20°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
Sensitive | Easily absorbing moisture |
Refractive Index | 1.722 |
Use | Every inhibitor of serine/hydroxybutyrate |
In vitro study | Enzastaurin blocks the proliferation of U87MG glioblastoma cells, PC-3 prostate cancer cells, and HCT116 colon cancer cells. When the concentration of Enzastaurin is lower than 1 M, it may have a mild induction of HCT116 and U87MG cells. Enzastaurin blocks the proliferation of many cell lines such as K-562, MOLT-4, HOP-92, and PC-3 cell lines. When the concentration of Enzastaurin is 4 μm, it can induce apoptosis of HCT116 colon cancer cells and U87MG malignant glioma cells. The apoptosis of HCT116 colon cancer cells induced by Enzastaurin was dose-dependent. Treatment of HCT116 cells with 4 μm Enzastaurin increased TUNEL positive cells from 2% to more than 50% at the basic level. In vivo studies showed that Enzastaurin significantly blocked the growth of HCT116 colon cancer cells and U87MG malignant glioma cells. Apoptosis of malignant lymphocytes in cutaneous T-cell lymphoma with Enzastaurin. The combination of Enzastaurin and GSK3 inhibitors increases the level of cytotoxicity. AR-A014418 combination of Enzastaurin and GSK3 inhibitors increases β-catenin protein levels and β-catenin-regulated transcriptional levels. The combination of Enzastaurin and AR-A014418 blocks β-catenin-regulated transcription. In addition, the combination of Enzastaurin and AR-A014418 increased mRNA levels and CD44 expression. |
In vivo study | Treatment of xenograft tumors with Enzastaurin in combination with radiation produced a greater reduction in microvessel density than when used alone. The reduction in microvessel density was consistent with delayed tumor growth. |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
WGK Germany | 3 |
RTECS | UX9626850 |
HS Code | 29339900 |
biological activity | Enzastaurin (LY317615) is an effective PKCβ selective inhibitor with IC50 of 6 nM, which is 6 to 20 times stronger than PKCα, PKCγ and PKCε. Phase 3. Enzastaurin (LY317615) is an effective PKCβ selective inhibitor. IC50 is 6 nM in cell-free test, which is 6 to 20 times higher than that in PKCα,PKCγ and PKCε. Phase 3. |
Target | Value |
PKCβ (Cell-free assay) | 6 nM |
PKCα (Cell-free assay) | 39 nM |
PKCγ (Cell-free assay) | 83 nM |
PKCε (Cell-free assay) | 110 nM |