Biological Activity
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 |
| Storage | Store at -80°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 1217447-06-7 |
| PubChem ID | 71311821 |
| InChI Key | GJEFFRDWFVSCOJ-PXPMWPIZSA-N |
| Smiles | SC[C@H](N)CNC1=CC=C(C(N[C@H]([C@@](OC)=O)CCSC)=O)C(C2=CC=CC=C2)=C1.FC(F)(C(O)=O)F |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 2.81 | 5 |
Preparing Stock Solutions
The following data is based on the product molecular weight 561.64. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.78 mL | 8.9 mL | 17.8 mL |
| 5 mM | 0.36 mL | 1.78 mL | 3.56 mL |
| 10 mM | 0.18 mL | 0.89 mL | 1.78 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Lerner et al (1995) Ras CAAX peptidomimetic FTI-277 selectively blocks oncogenic Ras signaling inducing cytoplasic accumulation of inactive Ras-Raf complexes. J.Biol.Chem. 270 26802 PMID: 7592920
Sun et al (1999) Antitumour efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: combination therapy with the cytotoxic agents cisplatin, taxol and gemcitabine. Cancer Res. 59 4919 PMID: 10519405
Lerner et al (1995) Disruption of oncogenic K-Ras4B processing and signaling by a potent geranylgeranyltransferase I inhibitor. J.Biol.Chem. 10 26770 PMID:
Keywords: FTI 277, supplier, Prodrug, FTI, 276, 2406, farnesyltransferase, FTase, H-Ras, K-Ras, MAPK, anti-proliferative, antiproliferative, tumour, tumor, FTI277, Protein, Prenyltransferases, Post-translational, Modifications, Protein, Prenyltransferases, Tocris Bioscience
