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RO4929097

Chemical Structure : RO4929097

CAS No.: 847925-91-1

RO4929097 (RG 4733;RO 4929097)

Catalog No.: PC-42810Not For Human Use, Lab Use Only.

RO4929097 (RG 4733) is a potent, selective, orally active γ-secretase inhibitor with IC50 of 4 nM, inhibits Notch processing in the Notch cell-based reporter assay with IC50 of 5 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

RO4929097 (RG 4733) is a potent, selective, orally active γ-secretase inhibitor with IC50 of 4 nM, inhibits Notch processing in the Notch cell-based reporter assay with IC50 of 5 nM.
RO4929097 (RG 4733) displays >100-fold selectivity against a panel of 75 other proteins of various types including receptors, ion channels and enzymes.
RO4929097 (RG 4733) inhibits Notch processing in human tumor-derived cells, inhibits the production of ICN, reducing the expression of the downstream Notch target Hes1 in A549 cells.
RO4929097 (RG 4733) demonstrates in vivo efficacy in A549 xenograft model.

Physicochemical Properties

M.Wt 469.4045
Formula C22H20F5N3O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 49 mg/mL

Chemical Name/SMILES

Propanediamide, N1-[(7S)-6,7-dihydro-6-oxo-5H-dibenz[b,d]azepin-7-yl]-2,2-dimethyl-N3-(2,2,3,3,3-pentafluoropropyl)-

References

1. Debeb BG, et al. Breast Cancer Res Treat. 2012 Jul;134(2):495-510.

2. Kaur G, et al. Cancer Lett. 2016 Feb 28;371(2):225-39.

3. He W, et al. Mol Oncol. 2011 Jun;5(3):292-301.

4. Luistro L, et al. Cancer Res. 2009 Oct 1;69(19):7672-80.

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