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Gamma Secretase

RO4929097 (847925-91-1)

RO4929097 is a γ secretase inhibitor with IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively. Phase 2.

Not Intended for Therapeutic Use. For research use only.

CAS: 847925-91-1 Category

RO4929097 (847925-91-1) Description:

RO4929097, also known as RO04929097, is an orally bioavailable, small-molecule gamma secretase (GS) inhibitor with potential antitumor activity. Gamma secretase inhibitor RO4929097 binds to GS and blocks activation of Notch receptors, which may inhibit tumor cell proliferation. The integral membrane protein GS is a multi-subunit protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors, at residues within their transmembrane domains. Overexpression of the Notch signaling pathway has been correlated with increased tumor cell growth. In vitro: Decreases the amount of Aβ peptides secreted into the culture medium in HEK293 cells (EC50= 14 nM); Strongly inhibits Notch processing (EC50= 5 nM) in the Notch cell-based reporter assay In vivo: Oral injection of 3 to 60 mg/kg RO4929097 once daily or twice daily to nude mice bearing A549 NSCLC xenografts for either 7, 14, or 21 days of a 21-day schedule results in significant tumor growth inhibition compared with vehicle-treated animals. The tumor growth inhibition values ranges from 66% to 91%.

RO4929097 (847925-91-1) Specifications:

Product Name RO4929097
Synonyms R4733; R 4733; R-4733; RO4929097; RO-4929097; RO 4929097; RO04929097; RO-04929097; RO 04929097.
Chemical Names (S)-2,2-dimethyl-N1-(6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N3-(2,2,3,3,3-pentafluoropropyl)malonamide
Purity >98% (or refer to the Certificate of Analysis)
CAS Number 847925-91-1
Molecular Formula C22H20F5N3O3
Molecular Weight 469.40452
Monoisotopic Mass 469.142 g/mol
MDL number MFCD18384976
InChIKey OJPLJFIFUQPSJR-INIZCTEOSA-N
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
SMILES O=C(N[[email protected]]1C2=CC=CC=C2C3=CC=CC=C3NC1=O)C(C)(C)C(NCC(F)(F)C(F)(F)F)=O
Form Powder
Color Off-white
Solubility  Soluble in DMSO, not in water
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >5 years if stored properly
Handling Protect from air and light
Application An inhibitor of the γ secretase (GS) complex

 


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RIDADR NONH for all modes of transport

References:

  • 1: Huynh C, Poliseno L, Segura MF, Medicherla R, Haimovic A, Menendez S, Shang S, Pavlick A, Shao Y, Darvishian F, Boylan JF, Osman I, Hernando E. Correction: The Novel Gamma Secretase Inhibitor RO4929097 Reduces the Tumor Initiating Potential of Melanoma. PLoS One. 2011;6(11). doi: 10.1371/annotation/a89c089f-ae9d-4453-a314-37efd5efb126. Epub 2011 Nov 2. PubMed PMID: 22073133; PubMed Central PMCID: PMC3207494.
  • 2: Kolb EA, Gorlick R, Keir ST, Maris JM, Lock R, Carol H, Kurmasheva RT, Reynolds CP, Kang MH, Wu J, Houghton PJ, Smith MA. Initial testing (stage 1) by the pediatric preclinical testing program of RO4929097, a γ-secretase inhibitor targeting notch signaling. Pediatr Blood Cancer. 2011 Aug 16. doi: 10.1002/pbc.23290. [Epub ahead of print] PubMed PMID: 22052798.
  • 3: Huynh C, Poliseno L, Segura MF, Medicherla R, Haimovic A, Menendez S, Shang S, Pavlick A, Shao Y, Darvishian F, Boylan JF, Osman I, Hernando E. The novel gamma secretase inhibitor RO4929097 reduces the tumor initiating potential of melanoma. PLoS One. 2011;6(9):e25264. Epub 2011 Sep 29. PubMed PMID: 21980408; PubMed Central PMCID: PMC3182998.
  • 4: Wu J, Wiegand R, LoRusso P, Li J. 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. 2011 Jun 1;879(19):1537-43. Epub 2011 Mar 31. PubMed PMID: 21497565.
  • 5: He W, Luistro L, Carvajal D, Smith M, Nevins T, Yin X, Cai J, Higgins B, Kolinsky K, Rizzo C, Packman K, Heimbrook D, Boylan JF. High tumor levels of IL6 and IL8 abrogate preclinical efficacy of the γ-secretase inhibitor, RO4929097. Mol Oncol. 2011 Jun;5(3):292-301. Epub 2011 Jan 21. PubMed PMID: 21315665.

1 review for RO4929097 (847925-91-1)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The RO4929097 (847925-91-1) is high purity,also customer service is pretty nice !gotta try!!

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