ChemicalBook > CAS DataBase List > Enzastaurin (LY317615)
Enzastaurin (LY317615)
Enzastaurin (LY317615)
- CAS No.170364-57-5
- Chemical Name:Enzastaurin (LY317615)
- CBNumber:CB92128716
- Molecular Formula:C32H29N5O2
- Formula Weight:515.6
- MOL File:170364-57-5.mol
Enzastaurin (LY317615) Property
- Melting point 249-261℃
- Boiling point 767.2±60.0 °C(Predicted)
- Density 1.34
- RTECS UX9626850
- Flash point 417.8℃
- storage temp. -20°C
- solubility DMSO: soluble10mg/mL, clear (warmed)
- form powder
- pka 7.88±0.60(Predicted)
- color , light orange to dark orange-red
- 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.
- NCI Dictionary of Cancer Terms LY317615
- FDA UNII UC96G28EQF
- UNSPSC Code 12352200
- NACRES NA.77
Safety
-
Symbol(GHS)
- Signal wordWarning
- Hazard statements H302-H413
- Precautionary statements P273-P301+P312+P330
Enzastaurin (LY317615) Price
More Price(2)
- Brand: Sigma-Aldrich(India)
- Product number: SML0762
- Product name : Enzastaurin
- Purity: ≥98% (HPLC)
- Packaging: 5MG
- Price: ₹11506.98
- Updated: 2022/06/14
- Buy: Buy
- Brand: Sigma-Aldrich(India)
- Product number: SML0762
- Product name : Enzastaurin
- Purity: ≥98% (HPLC)
- Packaging: 25MG
- Price: ₹46374.3
- Updated: 2022/06/14
- Buy: Buy
Enzastaurin (LY317615) Chemical Properties,Usage,Production
- 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
- Uses PKCβ-selective inhibitor, suppresses angiogenesis.
- Uses Enzastaurin has been used in splicing analysis to study its effects on splicing of a mutated exon.
- Definition ChEBI: 3-(1-methyl-3-indolyl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-3-indolyl]pyrrole-2,5-dione is a member of indoles and a member of maleimides.
- Biochem/physiol Actions Enzastaurin is a potent and PKCβ preferring inhibitor. Also, Enzastaurin inhibits AKT and GSK3β. Enzastaurin acts as anti-angiogenic and antineoplastic agent.
-
in vivo
Treatment of xenografts with Enzastaurin and radiation produces greater reductions in density of microvessels than either treatment alone. The decrease in microvessel density corresponds to delayed tumor growth[3].
- IC 50 PKCβ: 6 nM (IC50); PKCα: 39 nM (IC50); PKCγ: 83 nM (IC50); PKCε: 110 nM (IC50)
- References 1) Graff et al. (2005), The protein kinase Cbeta-selective inhibitor, Enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts; Cancer Res. 65 7462 2) Rizvi et al. (2006) Enzastaurin (LY317615), a protein kinase Cβ inhibitor, inhibits the AKT pathway and induces apoptosis in multiple myeloma cell lines; Mol.Cancer Ther. 5 1783 3) Ouaret and Larsen (2014), Protein kinase Cβ inhibition by enzastaurin leads to mitotic missegregation and preferential cytotoxicity toward colorectal cancer cells with chromosomal instability (CIN); Cell Cycle 13 2697 4) Zestos et al. (2016), PKCβ Inhibitors Attenuate Amphetamine-Stimulated Dopamine Efflux; ACS Chem.Neurosci. 7 757 5) Stranahan et al. (2016), Blood-brain barrier breakdown promotes macrophage infiltration and cognitive impairment in leptin receptor-deficient mice; J.Cereb.Blood Flow Metab. 36 2108
Enzastaurin (LY317615) Preparation Products And Raw materials
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- ENZASTAURIN 恩扎妥林 |CAS 170364-57-5
- 恩扎妥林,10 MM DMSO 溶液
- ENZASTAURIN(LY317615),PKCΒ抑制剂
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- PKCΒ抑制剂(ENZASTAURIN)
- 3-(1-甲基-1H-吲哚-3-基)-4-(1-(1-(2-吡啶甲基)-4-哌啶基)-1H-吲哚-3-基)-1H-吡咯-2,5-二酮
- 恩扎妥林
- 因扎妥雷
- 3-(1-甲基-1H-吲哚-3-基)-4-(1-(1-(吡啶-2-基甲基)哌啶-4-基)-1H-吲哚-3-基)-1H-吡咯-2,5-二酮
- 恩扎妥林(LY317615)
- 170364-57-5
- Enzastaurin, 10 mM in DMSO
- Sotrastaurin Impurity 11
- Enzastaurin LY317615 LY-317615
- 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
- ENZASTAURIN HCL
- Ly317615
- Enzastaurin
- CS-1980
- 3-(1-methyl-1H-indol-3-yl)-4-(1-(1-(pyridin-2-ylmethyl)piperidin-4-yl)-1H-indol-3-yl)-1H-pyrrole-2
- Enzastaurin (LY317615) USP/EP/BP
- DB-102
- Enzastaurin, 98%, a potent PKCβ selective inhibitor
- 3-(1-Methyl-1H-indol-3-yl)-4-(1-(1-(pyridin-2-ylmethyl)-piperidin-4-yl)-1H-indol-3-yl)-1H-pyrr
- D04014
- 3-(1-Methyl-1H-indol-3-yl)-4-(1-(1-(pyridin-2-ylmethyl)-piperidin-4-yl)-1H-indol-3-yl)-1H-pyrrole
- LY317615/Enzstataurin
- LY317615 (Enzastaurin)
- Enzastaurine
- Enzastaurin ( LY317615 )
- 3-(1-Methyl-1H-indol-3-yl)-4-(1-(1-(2-pyridinylmethyl)-4-piperidinyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
- Enzastaurin,Enzstataurin,LY317615,170364-57-5,1H-Pyrrole-2,5-dione, 3-
- Unii-uc96G28eqf
- 1H-Pyrrole-2,5-dione, 3-(1-methyl-1H-indol-3-yl)-4-(1-(1-(2-pyridinylmethyl)-4-piperidinyl)-1H-indol-3-yl)-