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About This Item

Empirical Formula (Hill Notation):
C22H20F5N3O3
CAS Number:
Molecular Weight:
469.40
MDL number:
UNSPSC Code:
12352200
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Quality Level

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

SMILES string

O=C1[C@H](C2=C(C3=C(N1)C=CC=C3)C=CC=C2)NC(C(C)(C(NCC(F)(C(F)(F)F)F)=O)C)=O

Related Categories

Biochem/physiol Actions

Orally active, potent and selective gamma-secretase inhibitor with anti-cancer efficacy in vitro and in vivo.

RO4929097 is an orally active, potent and selective gamma-secretase (γ-secretase) inhibitor (IC50 = 4 nM) that blocks Aβ1-40 production (IC50 = 14 nM in APP-overexpressing HEK293) and suppresses Notch signaling (IC50 = 5 nM by reporter assays) with >100-fold selectivity over 75 other enzymes, receptors and ion channels. RO4929097 reduces the size of MDA-MB-468 soft agar colonies in cultures (100-250 nM) and effectively suppresses A549 NSCLC xenografts-derived tumor growth in mice in vivo (3-60 mg/kg bid or qd p.o.).

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