Enzastaurin

10 mg

Cat. No.: 19-P20

$99.00

Enzastaurin inhibits PKCβ, PKCα, PKCγ and PKCε with IC50’s of 0.006, 0.039, 0.083 and 0.110 µM, respectively. It has a direct effect on human tumor cells by inducing apoptosis and suppressing the proliferation of cultured tumor cells. Enzastaurin suppresses VEGF-induced angiogenesis in the rat corneal micropocket assay and decreases microvessel density. It also prevents VEGF secretion from human tumor cell xenographs in nude mice. Prolonged courses of Enzastaurin increases chemotherapy or radiation tumor growth delay of breast, glioma and small cell lung cancer xenographs.

 

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TECHNICAL INFORMATION

Other Names: LY317615, D04014  

Chemical Formula:  C32H29N5O2

CAS Number: 170364-57-5

Molecular Weight: 515.6

Purity:  >99%

Appearance:  Red/orange solid 

Solubility: DMSO

 

STORAGE AND HANDLING

Storage: Store at 4°C and protected from light. Following reconstitution, store  aliquots at -20°C. 

Stability: Stock solutions stable at -20°C for up to 2 years.

Shipping Conditions: Shipped at room temperature.

 

PRODUCT USE

Soluble in DMSO at 7.1 mg/ml. If precipitate is observed,  vortex for 5 minutes. For most cells, the maximum tolerance to DMSO is less than 0.5%.

 

References

Podar et al. (2007) Targeting PKC in multiple myeloma: in vitro and in vivo effects of the novel | orally available small-molecule inhibitor enzastaurin (LY317615.HCl). Blood. 109(4):1669–1677.

Graff et al. (2005) The Protein Kinase Cβ–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.

Meng et al. (2010) Protein kinase Cbeta modulates ligand-induced cell surface death receptor accumulation: a mechanistic basis for enzastaurin-death ligand synergy. J Biol Chem. 285(2):888-902.

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