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ICONC13621 Enzastaurin(LY317615) (170364-57-5)
 
 
Catalog No.: C13621
CAS No.: 170364-57-5
Synonym: D04014
Chemical Name:

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

Molecular Formula:

C32H29N5O2

Molecular Weight: 515.60
 
Technical Data:
Appearance:
Solubility: Soluble in DMSO
Purity: >99%
Storage: at -20℃ 2 years
Original QC Data:
Shipping Conditions: Ambient Temp.
 
Price and Availability of Enzastaurin(LY317615):

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Biological Activity:

Enzastaurin induced marked dose-dependent growth inhibition 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.IC50 ranged from 0.6 to 1.6 μM.
Enzastaurin has a direct effect on human tumor cells, inducing apoptosis and suppressing the proliferation of cultured tumor cells. Enzastaurin treatment also suppresses the phosphorylation of GSK3ßser9, ribosomal protein S6S240/244, and AKTThr308.
Enz inhibited PKCβ and radiosensitized HDMEC with an enhancement ratio of 1.31 ± 0.05. Enz combined with RT reduced HDMEC capillary sprouting to a greater extent than either agent alone. Enz prevented radiation-induced GSK3β phosphorylation of serine 9 while having no direct effect on VEGFR phosphorylation. Treatment of xenografts with Enz and radiation produced greater reductions in microvessel density than either treatment alone. The reduction in microvessel density corresponded with increased tumor growth delay.

 
References:
1. Graff JR, et al. Cancer Res, 2005, 65(16), 7462-7469.

2. Rovedo MA, et al. J Invest Dermatol, 2011, 131(7), 1442-1449.

 
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