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Enzastaurin (LY317615)

Product Name
Enzastaurin (LY317615)
CAS No.
170364-57-5
Chemical Name
Enzastaurin (LY317615)
Synonyms
Enzastaurin;Ly317615;ENZASTAURIN HCL;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;D04014;DB-102;CS-1980;Enzastaurine;Unii-uc96G28eqf;LY317615/Enzstataurin
CBNumber
CB92128716
Molecular Formula
C32H29N5O2
Formula Weight
515.6
MOL File
170364-57-5.mol
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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.
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Safety

Hazard Codes 
Xn
Risk Statements 
22
WGK Germany 
3
HS Code 
29339900
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H413May cause long lasting harmful effects to aquatic life

Precautionary statements

P273Avoid release to the environment.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0762
Product name
Enzastaurin
Purity
≥98% (HPLC)
Packaging
5mg
Price
$127
Updated
2024/03/01
Sigma-Aldrich
Product number
SML0762
Product name
Enzastaurin
Purity
≥98% (HPLC)
Packaging
25mg
Price
$482
Updated
2024/03/01
Alfa Aesar
Product number
J67480
Product name
Enzastaurin, 99%
Packaging
10mg
Price
$152
Updated
2023/06/20
Alfa Aesar
Product number
J67480
Product name
Enzastaurin, 99%
Packaging
25mg
Price
$280
Updated
2023/06/20
Cayman Chemical
Product number
11601
Product name
Enzastaurin
Purity
≥98%
Packaging
5mg
Price
$86
Updated
2024/03/01
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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.

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

Raw materials

Preparation Products

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View Lastest Price from Enzastaurin (LY317615) manufacturers

Zhuozhou Wenxi import and Export Co., Ltd
Product
Enzastaurin (LY317615) 170364-57-5
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-06-27
Career Henan Chemical Co
Product
Enzastaurin 170364-57-5
Price
US $1.00/KG
Min. Order
1g
Purity
Min98% HPLC
Supply Ability
g/kg /ton
Release date
2019-12-20

170364-57-5, Enzastaurin (LY317615)Related Search:


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  • 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
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