RO4929097

2 mg

Cat. No.: 80-Y15

$169.00

RO4929097 is a small molecule gamma secretase inhibitor with an IC₅₀ of 4nM. It binds to gamma secretase and blocks the activation of Notch receptors, which may inhibit tumor cell proliferation. RO4929097 inhibits Notch processing in tumor cells as measured by the reduction of intracellular Notch expression by Western blot. RO4929097 produces a less transformed and flattened slower-growing phenotype but does not induce apoptosis or block tumor cell proliferation.

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TECHNICAL INFORMATION

Other Names: RO-4929097

Chemical Formula:  C22H20F5N3O3

CAS Number: 847925-91-1

Molecular Weight: 469.4

Purity:  >99%

Appearance:  white 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. If precipitate is observed,  vortex for 5 minutes.

 

References

Luistro et al. (2009) Preclinical profile of a potent gamma-secretase inhibitor targeting notch signaling with in vivo efficacy and pharmacodynamic properties. Cancer Res. 69(19):7672-80.

Wu et al. (2011) Validation and implementation of a liquid chromatography/tandem mass spectrometry assay for quantitation of the total and unbound RO4929097 | a γ-secretase inhibitor targeting Notch signaling | in human plasma. J Chromatogr B Analyt Technol Biomed Life Sci. 879(19):1537-43.

He et al. (2011) High tumor levels of IL6 and IL8 abrogate preclinical efficacy of the γ-secretase inhibitor | RO4929097. Mol Oncol. 5(3):292-301.

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