FTI 276 TFA |
カタログ番号GC36085
One-Click Copy Product Info
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FTI-276は、プラズモジウム・ファルシパルムと人間に対してそれぞれIC50値が0.9nMおよび0.5nMのタンパク質フェニルトランスフェラーゼ（PFT）阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1217471-51-6
Sample solution is provided at 25 µL, 10mM.
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FTI 276 TFA is a protein farnesyl transferase (PFT) inhibitor with an IC50 value of 1nM [1]. FTI 276 TFA can block Ras oncogenic signaling and prevent constitutive activation of the MAPK cascade [2]. FTI 276 TFA has been widely used to inhibit tumor growth in the primary mouse lung tumor model [3].
In vitro, FTI 276 TFA treatment (50μM) for 24 hours significantly reduced the extracellular MMP-1 level in 143B cells and inhibited the invasion of 143B cells[4].
In vivo, FTI 276 TFA treatment via daily intraperitoneal injection at a dose of 70mg/kg for 80 days significantly inhibited the growth of A549 xenograft tumors (express K-Ras mutations) in mice[5]. Intravenous infusion of 307μg/kg/day dose of FTI 276 TFA for 3 weeks significantly reduced myocardial fibrosis and improved cardiac remodeling in spontaneously hypertensive rats [6]. Continuous intraperitoneal injection of 50mg/kg/day dose of FTI 276 TFA for 36 consecutive days significantly inhibited tumor growth in the Calu-1 xenograft mouse model[7].
References:
[1] Chakrabarti D, Da Silva T, Barger J, et al. Protein Farnesyltransferase and Protein Prenylation inPlasmodium falciparum[J]. Journal of Biological Chemistry, 2002, 277(44): 42066-42073.
[2] Lerner E C, Qian Y, Blaskovich M A, et al. Ras CAAX peptidomimetic FTI-277 selectively blocks oncogenic Ras signaling by inducing cytoplasmic accumulation of inactive Ras-Raf complexes[J]. Journal of Biological Chemistry, 1995, 270(45): 26802-26806.
[3] Lantry L E, Zhang Z, Crist K A, et al. Chemopreventive efficacy of promising farnesyltransferase inhibitors[J]. Experimental lung research, 2000, 26(8): 773-790.
[4] Garamszegi N, Garamszegi S P, Scully S P. Matrix metalloproteinase‐1 contribution to sarcoma cell invasion[J]. Journal of cellular and molecular medicine, 2012, 16(6): 1331-1341.
[5] Sun J, Qian Y, Hamilton A D, et al. Both farnesyltransferase and geranylgeranyltransferase I inhibitors are required for inhibition of oncogenic K-Ras prenylation but each alone is sufficient to suppress human tumor growth in nude mouse xenografts[J]. Oncogene, 1998, 16(11): 1467-1473.
[6] Li X, Han J, Li L, et al. Effect of farnesyltransferase inhibition on cardiac remodeling in spontaneously hypertensive rats[J]. International journal of cardiology, 2013, 168(4): 3340-3347.
[7] Sun J, Qian Y, Hamilton A D, et al. Ras CAAX peptidomimetic FTI 276 selectively blocks tumor growth in nude mice of a human lung carcinoma with K-Ras mutation and p53 deletion[J]. Cancer research, 1995, 55(19): 4243-4247.
| Cell experiment [1]: | |
Cell lines | 143B cells |
Preparation Method | 143B cells were cultivated in DMEM medium supplemented with 10% heat-inactivated fetal bovine serum (FBS) at 37°C in an incubator with 5% CO2. After trypsinization, cells were quenched in DMEM with 5% bovine serum albumin then incubated overnight in p100 plates at 37°C to achieve a 70% confluence before serum starvation. Different concentrations of FTI 276 TFA (0, 2.5, 5, 15, and 50μM) were used in serum-free DMEM for 24h. Following exposure, cells were washed with PBS and harvested on ice for analysis. |
Reaction Conditions | 0, 2.5, 5, 15, and 50μM; 24h |
Applications | FTI 276 TFA treatment significantly reduced the extracellular MMP-1 protein levels in 143B cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female nude mice |
Preparation Method | Female nude mice (8 weeks old) were maintained in a controlled environment at 22±3°C and 60% relative humidity under a 12h light/dark cycle, and were given free access to standard rodent nutrition and water. Calu-1 cells were harvested, resuspended in PBS, and injected s.c. into the right and left flanks of mice (107 cells/flank). On day 32, after s.c. implantation of tumors, animals were dosed i.p. with 0.2ml once daily for 36 days. Control mice received a saline vehicle whereas treated mice received injections of FTI 276 TFA (50mg/kg). The tumor volumes were determined by measuring the length (1) and width (w) and calculating the volume (V = lw2/2). |
Dosage form | 50mg/kg/day for 36 days; i.p. |
Applications | FTI 276 TFA treatment significantly inhibited tumor growth in the Calu-1 xenograft mouse model. |
References: | |
| Cas No. | 1217471-51-6 | SDF | |
| Canonical SMILES | O=C(O)[C@@H](NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=CC=CC=C2)=O)CCSC.O=C(O)C(F)(F)F | ||
| Formula | C23H28F3N3O5S2 | M.Wt | 547.61 |
| 溶解度 | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8261 mL | 9.1306 mL | 18.2612 mL |
| 5 mM | 365.2 μL | 1.8261 mL | 3.6522 mL |
| 10 mM | 182.6 μL | 913.1 μL | 1.8261 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)