[CAS NO. 170364-57-5] Enzastaurin

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PRODUCTS SPECIFICATIONS [170364-57-5]

Catalog

HY-10342

Brand

MCE

CAS

170364-57-5

DESCRIPTION [170364-57-5]

Overview

MDL	MFCD11040980
Molecular Weight	515.61
Molecular Formula	C32H29N5O2
SMILES	O=C(C(C1=CN(C)C2=C1C=CC=C2)=C3C4=CN(C5CCN(CC6=NC=CC=C6)CC5)C7=C4C=CC=C7)NC3=O

For research use only. We do not sell to patients.

7 Publications Citing Use of MCE

Summary

Enzastaurin (LY317615) is a potent and selective PKCβ inhibitor with an IC ₅₀ of 6 nM, showing 6- to 20-fold selectivity over PKCα , PKCγ and PKCε ^[1] .

IC50 & Target

PKCβ

6 nM (IC ₅₀ )

PKCα

39 nM (IC ₅₀ )

PKCγ

83 nM (IC ₅₀ )

PKCε

110 nM (IC ₅₀ )

In Vitro

Enzastaurin (LY317615) application results in a marked dose-dependent inhibition of growth in all MM cell lines investigated, including MM.1S, MM.1R, RPMI 8226 (RPMI), RPMI-Dox40 (Dox40), NCI-H929, KMS-11, OPM-2, and U266, with IC ₅₀ from 0.6-1.6 μM. Enzastaurin direct impacts human tumor cells, inducing apoptosis and suppressing proliferation in cultured tumor cells. Enzastaurin also suppresses the phosphorylation of GSK3βser9, ribosomal protein S6S240/244, and AKTThr308 while having no direct effect on VEGFR phosphorylation ^[1] .
Enzastaurin increases apoptosis in malignant lymphocytes of CTCL. When combined with GSK3 inhibitors, enzastaurin demonstrates an enhancement of cytotoxicity levels. Treatment with a combination of enzastaurin and the GSK3 inhibitor AR-A014418 leads to increased levels of β-catenin total protein and β-catenin-mediated transcription. Blocking of β-catenin-mediated transcription or small hairpin RNA (shRNA) knockdown of β-catenin induces the same cytotoxic effects as that of enzastaurin plus AR-A014418. Additionally, treatment with enzastaurin and AR-A014418 decreases the mRNA levels and surface expression of CD44 ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00586508	Eli Lilly and Company\|Genentech, Inc.	Recurrent Glioblastoma	November 2007	Phase 2
NCT00415363	Eli Lilly and Company	Non Small Cell Lung Cancer\|Small Cell Lung Cancer	December 2006	Phase 2
NCT03776071	Denovo Biopharma LLC	Glioblastoma	December 16, 2020	Phase 3
NCT00718419	Eli Lilly and Company	Waldenstrom´s Macroglobulinemia\|Multiple Myeloma	July 2008	Phase 2
NCT00437268	Eli Lilly and Company	Colorectal Cancer\|Colorectal Carcinoma\|Colorectal Tumor	March 2007	Phase 2
NCT00530621	Eli Lilly and Company	Non-small Cell Lung Cancer	September 2007	Phase 2
NCT00685633	Eastern Cooperative Oncology Group\|National Cancer Institute (NCI)	Prostate Cancer	December 2008	Phase 2
NCT00451555	Eli Lilly and Company	Breast Cancer	April 11, 2007	Phase 2
NCT00309140	Eli Lilly and Company	Neoplasms\|Cancer	March 2006	Phase 2
NCT00105092	Eli Lilly and Company	Non-Small-Cell Lung Carcinoma	March 2005	Phase 2
NCT00466440	Eli Lilly and Company	Prostate Cancer	June 2007	Phase 2
NCT00451178	Eli Lilly and Company	Lymphoma	May 2007	Phase 2
NCT00709995	Eli Lilly and Company	Metastatic Renal Cell Carcinoma	June 30, 2008	Phase 2
NCT00420381	Eli Lilly and Company\|Gynecologic Oncology Group	Ovarian Cancer\|Neoplasms\|Carcinoma	January 2007	Phase 2
NCT00088205	Eli Lilly and Company	Mantle-Cell Lymphoma	March 2004	Phase 2
NCT01432951	Eli Lilly and Company	Solid Tumor\|Lymphoma, Malignant	November 2011	Phase 1
NCT00542919	Eli Lilly and Company	T-Cell Lymphoma\|B-Cell Lymphoma	November 2007	Phase 2
NCT00452257	Eli Lilly and Company	Leukemia, Lymphocytic	May 2007	Phase 1
NCT00192114	Eli Lilly and Company	Colonic Neoplasms	August 2005	Phase 2
NCT00308750	Eli Lilly and Company	Non-Small Cell Lung Cancer	March 2006	Phase 2
NCT00414960	Eli Lilly and Company	Lung Cancer	December 2007	Phase 2
NCT00469976	Eastern Cooperative Oncology Group\|National Cancer Institute (NCI)	Lung Cancer	June 2007	Phase 2
NCT00402116	Eli Lilly and Company\|University of California, San Francisco	Glioblastoma\|Glioblastoma Multiforme\|Gliosarcoma	September 2006	Phase 1\|Phase 2
NCT00042666	Eli Lilly and Company	Non-Hodgkin´s Lymphoma	June 2002	Phase 2
NCT00475644	Eli Lilly and Company	Lymphoma, Follicular	May 2007	Phase 2
NCT01388335	Eli Lilly and Company	Solid Tumor\|Lymphoma, Malignant	August 2011	Phase 1
NCT00744991	Eli Lilly and Company	Cutaneous T-Cell Lymphoma	September 2008	Phase 2
NCT00437294	Eli Lilly and Company	Breast Cancer	March 2007	Phase 2
NCT00108056	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	Glioma	April 7, 2005	Phase 1
NCT00295815	Eli Lilly and Company	Glioblastoma	January 2006	Phase 3
NCT00536939	Eli Lilly and Company\|Genentech, Inc.	Breast Cancer	November 2007	Phase 2
NCT00428714	Eli Lilly and Company	Prostate Cancer	January 2007	Phase 2
NCT00436280	Eli Lilly and Company	Lymphoma, Large Cell, Diffuse	February 2007	Phase 2
NCT00533429	Eli Lilly and Company\|Genentech, Inc.	Non-small Cell Lung Cancer	October 2007	Phase 2
NCT00386087	Eli Lilly and Company	Breast Neoplasms	November 2006	Phase 2
NCT00550927	Eli Lilly and Company\|National Cancer Institute (NCI)	Unspecified Adult Solid Tumor, Protocol Specific	November 2006	Phase 1
NCT00612586	Eli Lilly and Company\|Roche Pharma AG	Colorectal Cancer	February 2008	Phase 2
NCT00391118	Eli Lilly and Company	Ovarian Cancer\|Fallopian Tube Neoplasms\|Peritoneal Neoplasm	November 2006	Phase 2
NCT00452413	Eli Lilly and Company	Non-Small Cell Lung Cancer\|Malignant Solid Tumor	May 2007	Phase 1\|Phase 2
NCT00509821	Eli Lilly and Company	Glioblastoma Multiforme	October 2007	Phase 2
NCT00332202	Eli Lilly and Company	Non Hodgkin Lymphoma	June 2006	Phase 3
NCT00516607	European Organisation for Research and Treatment of Cancer - EORTC	Brain and Central Nervous System Tumors	July 2007	Phase 1
NCT05463679	Aytu BioPharma, Inc.\|Parexel	Vascular Ehlers-Danlos Syndrome	January 2024	Phase 3
NCT00538681	Eli Lilly and Company	Lung Cancer	September 2007	Phase 2
NCT01445119	Eli Lilly and Company\|National Cancer Institute (NCI)	Recurrent Gliomas	January 2007	Phase 1
NCT00503724	Pediatric Brain Tumor Consortium\|National Cancer Institute (NCI)	Brain and Central Nervous System Tumors\|Neuroblastoma	June 2007	Phase 1
NCT00407758	Gynecologic Oncology Group\|National Cancer Institute (NCI)\|GOG Foundation	Ovarian Cancer\|Primary Peritoneal Cavity Cancer	November 2006	Phase 2
NCT03263026	Denovo Biopharma LLC	Diffuse Large B-Cell Lymphoma	March 20, 2018	Phase 3
NCT00190723	Eli Lilly and Company	Malignant Glioma	October 2002	Phase 2
NCT00052273	Jonsson Comprehensive Cancer Center\|Eli Lilly and Company	Adult\|Solid Tumor	December 2002	Phase 1
NCT00267020	Eli Lilly and Company	Pancreatic Neoplasm	December 2005	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 8.33 mg/mL ( 16.16 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9395 mL	9.6973 mL	19.3945 mL
5 mM	0.3879 mL	1.9395 mL	3.8789 mL
10 mM	0.1939 mL	0.9697 mL	1.9395 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 0.83 mg/mL (1.61 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 0.83 mg/mL (1.61 mM); Suspended solution; Need ultrasonic

* All of the co-solvents are available by MCE.

References

Synonyms

1H-Pyrrole-2,5-dione, 3-(1-methyl-1H-indol-3-yl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-1H-indol-3-yl]-

3-(1-Methyl-1H-indol-3-yl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione

Enzastaurin

3-(1-Methyl-1H-indol-3-yl)-4-[1-[1-[(pyridin-2-yl)methyl]piperidin-4-yl]-1H-indol-3-yl]pyrrole-2,5-dione

3-(1-Methylindol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]indol-3-yl]pyrrole-2,5-dione

DB 102