FTI 277

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Cat.No. 2407 - FTI 277 | C22H29N3O3S2.C2HF3O2 | CAS No. 1217447-06-7
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% (HPLC)
Datasheet
Citations
Reviews
Literature (1)

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.05 mM 35.61 mL 178.05 mL 356.1 mL
0.25 mM 7.12 mL 35.61 mL 71.22 mL
0.5 mM 3.56 mL 17.8 mL 35.61 mL
2.5 mM 0.71 mL 3.56 mL 7.12 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

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, Tax. and gemcit. 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


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Keywords: FTI 277, 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, 2407, Tocris Bioscience

Citations for FTI 277

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Literature in this Area

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