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FTI 277

Catalog #: 2407
1 Citation Datasheet / COA / SDS

Discontinued Product

2407 has been discontinued.
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FTI 277 | CAS No. 1217447-06-7 | Other Transferase Inhibitors
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Description: Prodrug form of FTI 276 (Cat. No. 2406)

Chemical Name: N-[4-[2(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl]methionine methyl ester trifluoroacetate salt

Purity: ≥95%

Product Details
Citations (1)
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Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

FTI 277 is a prodrug form of FTI 276 (Cat. No. 2406) that inhibits farnesyltransferase (FTase) (IC50 = 0.5 nM). Inhibits H-Ras and K-Ras processing in whole cells (IC50 values are 0.1 and 10 μM respectively) and disrupts constitutive H-Ras-specific activation of MAPK. Causes significant antiproliferative effects in human malignant glioma cells and many other tumor cell lines.

Technical Data

M.Wt:
561.64
Formula:
C22H29N3O3S2.C2HF3O2
Solubility:
Soluble to 5 mM in water
Purity:
≥95%
Storage:
Store at -80°C
CAS No:
1217447-06-7

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Ras CAAX peptidomimetic FTI-277 selectively blocks oncogenic Ras signaling inducing cytoplasic accumulation of inactive Ras-Raf complexes.
    Lerner et al.
    J.Biol.Chem., 1995;270:26802
  2. Disruption of oncogenic K-Ras4B processing and signaling by a potent geranylgeranyltransferase I inhibitor.
    Lerner et al.
    J.Biol.Chem., 1995;10:26770
  3. Antitumour efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: combination therapy with the cytotoxic agents cisplatin, Tax. and gemcit.
    Sun et al.
    Cancer Res., 1999;59:4919

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Citation for FTI 277

The citations listed below are publications that use Tocris products. Selected citations for FTI 277 include:

1 Citation: Showing 1 - 1

  1. ABL allosteric inhibitors synergize with statins to enhance apoptosis of metastatic lung cancer cells.
    Authors: Luttman Et al.
    Cell Rep.  2021;37:109880

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