An inhibitor of γ-secretase
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Ro 4929097

Item No. 19996

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N1-[(7S)-6,7-dihydro-6-oxo-5H-dibenz[b,d]azepin-7-yl]-2,2-dimethyl-N3-(2,2,3,3,3-pentafluoropropyl)-propanediamide
CAS Number
847925-91-1
Molecular Formula
C22H20F5N3O3
Formula Weight
469.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS(pH 7.2)(1:1): 0.1 mg/mlDMSO: 15 mg/mlEthanol: 10 mg/ml
λmax
230 nm
SMILES
O=C(C(C)(C)C(NCC(F)(F)C(F)(F)F)=O)N[C@@H]1C(NC2=C(C=CC=C2)C3=C1C=CC=C3)=O
InChi Code
InChI=1S/C22H20F5N3O3/c1-20(2,18(32)28-11-21(23,24)22(25,26)27)19(33)30-16-14-9-4-3-7-12(14)13-8-5-6-10-15(13)29-17(16)31/h3-10,16H,11H2,1-2H3,(H,28,32)(H,29,31)(H,30,33)/t16-/m0/s1
InChi Key
OJPLJFIFUQPSJR-INIZCTEOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

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    1 mg

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    5 mg

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    10 mg

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    Cayman Chemical
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    Product Description

    Ro 4929097 is a potent inhibitor of γ-secretase (IC50 = 4 nM) that blocks both Aβ40 and Notch processing (IC50s = 14 and 5 nM, respectively).1 It displays greater than 100-fold selectivity for γ-secretase over a panel of 75 other enzymes, receptors, and ion channels. Ro 4929097 does not block tumor cell growth or induce apoptosis but instead produces a less transformed, flattened, slower-growing phenotype.1 It is orally active against cancer xenograft models, altering gene expression related to angiogenesis and cell differentiation.1 Ro 4929097 also reduces tumor initiating potential of melanoma cells in vivo by blocking Notch-dependent gene expression.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Luistro, L., He, W., Smith, M., et al. Preclinical profile of a potent gamma-secretase inhibitor targeting notch signaling with in vivo efficacy and pharmacodynamic properties. Cancer Res. 69(19), 7620-7680 (2009).

    2. Huynh, C., Poliseno, L., Segura, M.F., et al. The novel gamma secretase inhibitor RO4929097 reduces the tumor initiating potential of melanoma. PLoS One 6(9), (2011).