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Enzastaurin

Enzastaurin structure

CAS No:
170364-57-5
Formula:
C32H29N5O2
Chemical Name:
Enzastaurin
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
Categories:
Biochemical Engineering > Inhibitors

Description

Enzastaurin is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε.

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.|Enzastaurin, an investigational, targeted, oral agent, will be evaluated at more than 100 sites worldwide for the treatment of relapsed glioblastoma multiforme (GBM), an aggressive and malignant form of brain cancer.

Enzastaurin Basic Attributes

Molecular Weight：

515.6

Exact Mass：

515.60

UNII：

UC96G28EQF

DSSTox ID：

DTXSID5044029

HScode：

29339900

Characteristics

PSA：

72.2

XLogP3：

3.7

Appearance：

light orange to dark orange-red

Density：

1.34

Melting Point：

154-156 °C

Boiling Point：

767.2±60.0 °C(Predicted)

Flash Point：

417.8℃

Refractive Index：

1.723

Water Solubility：

DMSO: soluble10mg/mL, clear (warmed)

Storage Conditions：

-20°C

Vapor Pressure：

1.87E-23mmHg at 25°C

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

hazard class code：

RTECS Number：

UX9626850

Marks：

Precautionary statement(s)：

P264, P270, P273, P301+P312, P330, P501

Hazard Statements：

H302-H413

Drug Information

Drug Indication：

Investigated for use/treatment in brain cancer, lymphoma (non-hodgkin's), and lung cancer.

Mechanism of Action：

Enzastaurin is an oral serine-threonine kinase inhibitor that is designed to suppress tumor growth through multiple mechanisms. Preclinical data indicate it may reduce the cell's ability to reproduce (cell proliferation), increase the natural death of the tumor cells (apoptosis), and inhibit tumor- induced blood supply (angiogenesis). Enzastaurin has been shown to inhibit signaling through the PKC-B and PI3K/AKT pathways. These pathways have been shown to be activated in a wide variety of cancers. In addition to glioblastoma, enzastaurin is also being studied in multiple other tumor types, including non-Hodgkin's lymphoma, colorectal cancer, non-small cell lung cancer, pancreatic cancer, and mantle cell lymphoma.

MeSH Entry Terms：

enzastaurin

Enzastaurin Use and Manufacturing

PKCβ-selective inhibitor, suppresses angiogenesis.

Computed Properties

Molecular Weight:515.6
XLogP3:3.7
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:4
Rotatable Bond Count:5
Exact Mass:515.23212518
Monoisotopic Mass:515.23212518
Topological Polar Surface Area:72.2
Heavy Atom Count:39
Complexity:974
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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