| Size | Price | Stock | Qty |
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| 10mg |
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| Other Sizes |
| Targets |
FTI 276 TFA targets protein farnesyl transferase (PFT), a zinc-containing heterodimeric enzyme that catalyzes the transfer of a farnesyl group from farnesyl pyrophosphate to the cysteine residue of the C-terminal CAAX motif of substrate proteins. Key substrates include Ras family proteins (K-Ras, N-Ras, H-Ras), which are critical regulators of cell proliferation, differentiation, and survival. By inhibiting PFT, FTI 276 blocks the membrane localization and function of farnesylated proteins, thereby disrupting oncogenic signaling pathways. The compound shows potent activity against both human and Plasmodium falciparum farnesyl transferase, with IC₅0 values of 0.5 nM and 0.9 nM, respectively.
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| ln Vitro |
In vitro, FTI 276 TFA potently inhibits protein farnesyl transferase activity with IC₅0 values of 0.5 nM for the human enzyme and 0.9 nM for the Plasmodium falciparum enzyme. The compound demonstrates concentration-dependent inhibition of farnesylation of Ras and other CAAX-containing proteins. In cellular assays, FTI 276 treatment leads to the accumulation of unprocessed Ras proteins, disruption of Ras membrane localization, and inhibition of Ras-mediated signaling pathways including the MAPK and PI3K/AKT pathways. The compound exhibits antiproliferative activity against various cancer cell lines and shows activity against malaria parasites.
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| ln Vivo |
In vivo, FTI 276 has been studied in preclinical models of cancer and parasitic infections. As a protein farnesyl transferase inhibitor, the compound blocks the farnesylation of Ras and other proteins, leading to inhibition of tumor growth and angiogenesis. The compound has been evaluated in animal models of malaria, showing activity against Plasmodium falciparum. FTI 276's potent inhibition of both human and parasitic PFT makes it a valuable tool for studying the role of protein farnesylation in various disease contexts. However, specific in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources.
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| Enzyme Assay |
In vitro enzyme assays for FTI 276 TFA involve measuring protein farnesyl transferase activity using recombinant human or P. falciparum enzyme. The assay is performed in 96-well plates using a fluorescence-based or scintillation proximity assay format. The enzyme is incubated with a farnesyl pyrophosphate donor, a biotinylated peptide substrate (e.g., biotin-Ras CAAX peptide), and varying concentrations of FTI 276 (0.001-1000 nM) in assay buffer. After incubation at 37degC for 30-60 minutes, the reaction is stopped and the farnesylated product is captured on streptavidin-coated plates or beads. Quantification is performed by fluorescence or scintillation counting. IC₅0 values are determined from dose-response curves using nonlinear regression.
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| Cell Assay |
In vitro cellular assays for FTI 276 TFA are performed using cancer cell lines such as HeLa, MCF-7, or A549 cells. Cells are cultured in appropriate medium and seeded in 96-well plates. Cells are treated with serial dilutions of FTI 276 (0.001-10 microM) for 24-72 hours. Cell viability is measured using MTT or CellTiter-Glo assays. Ras processing and membrane localization are assessed by Western blotting, with farnesylated Ras appearing as a faster-migrating band compared to unprocessed Ras. Apoptosis is evaluated by caspase-3/7 activity and PARP cleavage. Cell cycle analysis is performed by flow cytometry. IC₅0 values for antiproliferative activity are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies for FTI 276 are conducted in xenograft mouse models of cancer or in malaria models. In tumor models, immunocompromised mice bearing subcutaneous xenografts of cancer cell lines are administered FTI 276 intraperitoneally or subcutaneously at doses determined by pharmacokinetic studies. Tumor volume and body weight are monitored. Ras processing in tumor tissues is assessed by Western blotting. In malaria models, mice infected with P. falciparum or P. berghei are treated with FTI 276, and parasitemia is monitored by blood smears. Efficacy is compared to vehicle control and standard-of-care agents.
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| ADME/Pharmacokinetics |
FTI 276 TFA (CAS#: 1217471-51-6) has molecular formula C23H2₈F3N3O₅S2 and molecular weight 547.61. The chemical name is (2S)-2-[(5-{[(2R)-2-amino-3-sulfanylpropyl]amino}-[1,1'-biphenyl]-2-yl)formamido]-4-(methylsulfanyl)butanoic acid; trifluoroacetic acid. The compound is a potent protein farnesyl transferase inhibitor with IC₅0 values of 0.5 nM (human) and 0.9 nM (P. falciparum). It is a research chemical for laboratory use only. Storage: powder at -20degC for up to 3 years. The compound is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Toxicological information for FTI 276 TFA is limited as the compound is a research chemical. Based on its mechanism of farnesyl transferase inhibition, potential toxicities may include effects on rapidly proliferating tissues, as farnesylation is essential for the function of many proteins involved in cell growth and survival. The compound should be handled with standard laboratory precautions including the use of personal protective equipment and working in a well-ventilated area. Avoid inhalation, ingestion, and skin contact. The compound should be stored at -20degC and disposed of according to institutional guidelines for chemical waste.
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| References | |
| Additional Infomation |
FTI 276 TFA (CAS#: 1217471-51-6) is a potent protein farnesyl transferase (PFT) inhibitor with IC₅0 values of 0.5 nM (human) and 0.9 nM (Plasmodium falciparum). Farnesyl transferase is a key enzyme in the post-translational modification of Ras and other CAAX-containing proteins, which are critical regulators of cell proliferation and survival. The compound is used in research to study the role of protein farnesylation in cancer, parasitic infections, and cell signaling. FTI 276 has been investigated as a potential anticancer and antimalarial agent. As of the current date, FTI 276 TFA remains a preclinical research compound and is not approved for clinical use.
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| Molecular Formula |
C23H28F3N3O5S2
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| Molecular Weight |
547.610733985901
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| Exact Mass |
547.142
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| CAS # |
1217471-51-6
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| Related CAS # |
FTI 276;170006-72-1
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| PubChem CID |
395753
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
36
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| Complexity |
601
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| Defined Atom Stereocenter Count |
2
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| SMILES |
S(C)CC[C@@H](C(=O)O)NC(C1C=CC(=CC=1C1C=CC=CC=1)NC[C@H](CS)N)=O.FC(C(=O)O)(F)F
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| InChi Key |
IAVHISGQCODLHL-WSCVZUBPSA-N
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| InChi Code |
InChI=1S/C21H27N3O3S2.C2HF3O2/c1-29-10-9-19(21(26)27)24-20(25)17-8-7-16(23-12-15(22)13-28)11-18(17)14-5-3-2-4-6-14;3-2(4,5)1(6)7/h2-8,11,15,19,23,28H,9-10,12-13,22H2,1H3,(H,24,25)(H,26,27);(H,6,7)/t15-,19+;/m1./s1
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| Chemical Name |
(2S)-2-[[4-[[(2R)-2-amino-3-sulfanylpropyl]amino]-2-phenylbenzoyl]amino]-4-methylsulfanylbutanoic acid;2,2,2-trifluoroacetic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~182.61 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.57 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.57 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8261 mL | 9.1306 mL | 18.2612 mL | |
| 5 mM | 0.3652 mL | 1.8261 mL | 3.6522 mL | |
| 10 mM | 0.1826 mL | 0.9131 mL | 1.8261 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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