Free shipping on all orders over $ 500

RO4929097

Cat. No. M2015
RO4929097 Structure
Size Price Availability Quantity
10mg USD 220 In stock
50mg USD 600 In stock
Bulk Inquiry?

Quality Control
Biological Activity

RO4929097 is a potent and selective inhibitor of gamma-secretase, with IC50 of 4 nM and also inhibits Aβ40 and ICN with EC50 of 14 nM and 5 nM, producing inhibitory activity of Notch signaling in tumor cells. RO4929097 inhibits Notch processing in tumor cells as measured by the reduction of intracellular Notch expression by Western blot. The RO4929097 IC50 in cell-free and cellular assays is in the low nanomolar range with >100-fold selectivity with respect to 75 other proteins of various types (receptors, ion channels, and enzymes). RO4929097 induced significant differences in event-free survival (EFS) distribution compared to control in 6 of 26 (23%) of the evaluable solid tumor xenografts and in 0 of 8 (0%) of the evaluable ALL xenografts. In human primary melanoma cell lines, RO4929097 decreased the levels of NOTCH transcriptional target HES1. Moreover, RO4929097 affected the growth of human primary melanoma xenograft in NOD/SCID/IL2gammaR-/- mice and inhibited subsequent tumor formation in a serial xenotransplantation model, suggesting that inhibition of NOTCH signaling suppresses the tumor initiating potential of melanoma cells. In addition, RO4929097 decreased tumor volume and blocked the invasive growth pattern of metastatic melanoma cell lines in vivo.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 469.4
Formula C22H20F5N3O3
CAS Number 847925-91-1
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
References

Phase I study of RO4929097, a gamma secretase inhibitor of Notch signaling, in patients with refractory metastatic or locally advanced solid tumors.
Tolcher AW, et al. J Clin Oncol. 2012 Jul 1;30(19):2348-53. PMID: 22529266.

Initial testing (stage 1) by the pediatric preclinical testing program of RO4929097, a γ-secretase inhibitor targeting notch signaling.
Kolb EA, et al. Pediatr Blood Cancer. 2012 May;58(5):815-8. PMID: 22052798.

The novel gamma secretase inhibitor RO4929097 reduces the tumor initiating potential of melanoma.
Huynh C, et al. PLoS One. 2011;6(9):e25264. PMID: 21980408.

Preclinical profile of a potent gamma-secretase inhibitor targeting notch signaling with in vivo efficacy and pharmacodynamic properties.
Luistro L, et al. Cancer Res. 2009 Oct 1;69(19):7672-80. PMID: 19773430.

Related Gamma-secretase Products
YO-01027

YO-01027 (Dibenzazepine, DBZ) is a dipeptidic γ-secretase inhibitor with IC50 of 2.6 nM and 2.9 nM for APPL and Notch cleavage, respectively.

LY900009

LY900009 is a potent Notch inhibitor with IC50 of 0.27 nM.

LY3039478

LY3039478 is a novel and orally bioavailable inhibitor of Notch-1 intracellular domain (N1ICD) cleavage with IC50 of ~1 nM.

FLI-06

FLI-06 is a novel inhibitor of Notch signaling with EC50 of 2.3 μM.

Semagacestat

Semagacestat (LY450139) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, respectively.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: RO4929097 supplier, Gamma-secretase, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.