Enzastaurin


Catalog No. size PriceQuantity
M6790-2 2mg solid $104
M6790-10 10mg solid $401

Description

Cas:170364-57-5 (free base)

Product Information

Enzastaurin, also known as DB-102 and LY317615, is a synthetic macrocyclic bisindolemaleimide 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 and so tumor burden.

 

Chemical Formula: C32H29N5O2

 

Exact Mass: 515.23213

 

Molecular Weight: 515.6

 

Elemental Analysis: C, 74.54; H, 5.67; N, 13.58; O, 6.21

 

Related CAS #:170364-57-5 (free base)  359017-79-1 (HCl)  365253-37-8 (2HCl)    

 

Synonym:

 

LY317615

LY-317615

D04014

LY317615

DB-102

DB102

Enzastaurin

Enzastaurin free base

 

Chemical Name:

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

 

InChi Key:

AXRCEOKUDYDWLF-UHFFFAOYSA-N

 

InChi Code:

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)

 

Smiles Code:

O=C(C(C1=CN(C)C2=C1C=CC=C2)=C3C4=CN(C5CCN(CC6=NC=CC=C6)CC5)C7=C4C=CC=C7)NC3=O

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

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 IC50 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.

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.

 

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.

 

References

 

  1. Civallero M, Cosenza M, Bari A, Sacchi S. Rational combinations of enzastaurin with novel targeted agents for patients with B-cell non-Hodgkin's lymphoma. Expert Opin Investig Drugs. 2011 Aug;20(8):1029-31. Epub 2011 Jun 25. PubMed PMID: 21702717.

 

  1. Bodo J, Sedlak J, Maciejewski JP, Almasan A, Hsi ED. HDAC inhibitors potentiate the apoptotic effect of enzastaurin in lymphoma cells. Apoptosis. 2011 Jun 11. [Epub ahead of print] PubMed PMID: 21667043.

 

  1. Schmidinger M, Szczylik C, Sternberg CN, Kania M, Kelly CS, Decker R, Hamid O, Faelker T, Escudier B. Dose Escalation and Pharmacokinetics Study of Enzastaurin and Sunitinib Versus Placebo and Sunitinib in Patients With Metastatic Renal Cell Carcinoma. Am J Clin Oncol. 2011 Jun 4. [Epub ahead of print] PubMed PMID: 21654314.

 

  1. Querfeld C, Kuzel TM, Kim YH, Porcu P, Duvic M, Musiek A, Rook AH, Mark LA, Pinter-Brown L, Hamid O, Lin B, Bian Y, Boye M, Day JM, Rosen ST. Multicenter phase II trial of enzastaurin in patients with relapsed or refractory advanced cutaneous T-cell lymphoma. Leuk Lymphoma. 2011 Aug;52(8):1474-80. Epub 2011 Jun 8. PubMed PMID: 21649541.

 

  1. Ysebaert L, Morschhauser F. Enzastaurin hydrochloride for lymphoma: reassessing the results of clinical trials in light of recent advances in the biology of B-cell malignancies. Expert Opin Investig Drugs. 2011 Aug;20(8):1167-74. Epub 2011 Jun 5. PubMed PMID: 21639821.

 

Products are for research use only. Not for human use.

 

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