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FTI277 (FTI-277) is a peptide mimetic of the COOH-terminal Cys-Val-Ile-Met of K-Ras4B which is a novel, potent and selective farnesyltransferase (FTase) inhibitor with antiviral activity. It inhibits FTase with an IC50 of 500 pM. It shows >100-fold selectivity for FTase over the closely related GGTase I. FTI-277 is a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling.FTI-277 inhibits the processing of both oncogenic and normal Ras. FTI-277 was extremely potent (IC50 = 100 nM) at inhibiting H-Ras, but not the geranylgeranylated Rap1A processing in whole cells.
ln Vitro |
Radioresistant cells expressing the 24-kDa isoform (HeLa 3A) showed a significant decrease in survival when treated with FTI-277 (20 μM) for 48 hours prior to irradiation; however, this treatment had no effect on the survival of control cells (HeLa PINA). In addition to decreasing G(2)/M-phase arrest in both cell types and stimulating postmitotic cell death in HeLa 3A cells, FTI-277 has a radiosensitizing effect[1]. PC-3 cell migration and invasion were reduced in a time- and dose-dependent manner upon treatment with GGTI-298 and FTI-277[3].
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ln Vivo |
When compared to vehicle alone, FTI-277 therapy inhibited elevated PTP-1B and PTEN protein expression in burned mice. Nevertheless, in sham-burned animals, FTI-277 had no discernible effect on PTP-1B or PTEN protein expression[2].
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Animal Protocol |
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References |
[1]. Cohen-Jonathan E, et al. The farnesyltransferase inhibitor FTI-277 suppresses the 24-kDa FGF2-induced radioresistance in HeLa cells expressing wild-type RAS. Radiat Res. 1999 Oct;152(4):404-11.
[2]. Nakazawa H, et al. Role of protein farnesylation in burn-induced metabolic derangements and insulin resistance in mouse skeletal muscle. PLoS One. 2015 Jan 16;10(1):e0116633. [3]. Virtanen SS, et al. Inhibition of GGTase-I and FTase disrupts cytoskeletal organization of human PC-3 prostate cancer cells. Cell Biol Int. 2010 Aug;34(8):815-26. |
Molecular Formula |
C₂₂H₂₉N₃O₃S₂
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Molecular Weight |
447.61
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CAS # |
170006-73-2
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Related CAS # |
FTI-277 hydrochloride;180977-34-8
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SMILES |
COC(=O)[C@H](CCSC)NC(=O)c1ccc(NC[C@@H](N)CS)cc1c2ccccc2
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InChi Key |
GKFPROVOIQKYTO-UZLBHIALSA-N
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InChi Code |
InChI=1S/C22H29N3O3S2/c1-28-22(27)20(10-11-30-2)25-21(26)18-9-8-17(24-13-16(23)14-29)12-19(18)15-6-4-3-5-7-15/h3-9,12,16,20,24,29H,10-11,13-14,23H2,1-2H3,(H,25,26)/t16-,20+/m1/s1
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Chemical Name |
L-Methionine, N-((5-((2-amino-3-mercaptopropyl)amino)(1,1'-biphenyl)-2-yl)carbonyl)-, methyl ester, (R)-
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Synonyms |
FTI277 FTI-277 FTI 277
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2341 mL | 11.1704 mL | 22.3409 mL | |
5 mM | 0.4468 mL | 2.2341 mL | 4.4682 mL | |
10 mM | 0.2234 mL | 1.1170 mL | 2.2341 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.