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Purity: ≥98%
FTI-2153 is a potent and selective farnesyltransferase (FTase) inhibitor, with an IC50 of 1.4 nM and with >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. FTI-2153 inhibits bipolar spindle formation during mitosis independently of transformation and Ras and p53 mutation status. FTI-2153 was reported to block bipolar spindle formation and chromosome alignment and causes prometaphase accumulation during mitosis of human lung cancer cells.
| ln Vitro |
Two human lung cancer cell lines that undergo mitosis are inhibited in the development of bipolar spindles by FTI-2153 [2]. In both transformed and untransformed cells, the fraction of pro-cells with dividing DNA shape is increased by FTI-2153 [2]. The proliferation of T-24 and Calu-1 cells was decreased by 38% and 36%, respectively, by FTI-2153 (15 μM). With an inhibition rate of 8%, the scaffolds of NIH3T3, HFF, and HT-1080 were less effective in inhibiting the growth of A-549 and OVCAR3 cells by 25% and 22%, respectively. Thus, although FTI-2153 decreased cell growth equally in T-24 and Calu-1 cells, it only inhibited Calu-8 and 13% of the cells in T-24. FTI-2153 inhibits the proliferation of both HFF and NIH3T3 cells, however only NIH3T3 cells are resistant to FTI-2153's ability to cause bipolar spindle formation [2]. 2]
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: NIH3T3, HFF, HT1080, T-24, OVCAR3, A-549 and Calu-1 cells. Tested Concentrations: 48 hrs (hours). Incubation Duration: 15 μM. Experimental Results: When A-549 cells were treated with FTI-2153 (15 μM, 48 hrs (hours)), the proportion of metaphase cells increased relative to other stages of mitosis. FTI-2153 accumulates cells with a rosette-like morphology during metaphase, in which chromosomes form rings around single-cell microtubules. In all cells, except T-24 and NIH3T3, FTI-2153 treatment increased the proportion of cells in metaphase mitosis and diminished the proportion of cells in telophase/mitosis. In HT1080 cells, the percentages of cells in prophase and telophase/cytokinesis were 5% and 85%, respectively, in control cells and 55% and 35%, respectively, in treated cells. Similar results were found in HFF cells. As mentioned previously, Calu-1 and A-549 cells had similarly large changes, whereas OVCAR3 had smaller changes. In contrast, FTI-2153 did not Dramatically affect the dist |
| References |
[1]. Sun J, et al. Antitumor 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. 1999 Oct 1;59(19):4919-26.
[2]. N C Crespo, et al. The farnesyltransferase inhibitor, FTI-2153, inhibits bipolar spindle formation during mitosis independently of transformation and Ras and p53 mutation status. Cell Death Differ. 2002 Jul;9(7):702-9. |
| Molecular Formula |
C25H30N4O3S
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| Molecular Weight |
466.595704555511
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| CAS # |
344900-92-1
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| Related CAS # |
FTI-2153 TFA;2820151-01-5
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| SMILES |
CSCC[C@@H](C(OC)=O)NC(C1=CC=C(CNCC2=CNC=N2)C=C1C3=CC=CC=C3C)=O
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| InChi Key |
KZCMMZOLCBZLNG-QHCPKHFHSA-N
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| InChi Code |
InChI=1S/C25H30N4O3S/c1-17-6-4-5-7-20(17)22-12-18(13-26-14-19-15-27-16-28-19)8-9-21(22)24(30)29-23(10-11-33-3)25(31)32-2/h4-9,12,15-16,23,26H,10-11,13-14H2,1-3H3,(H,27,28)(H,29,30)/t23-/m0/s1
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| Chemical Name |
L-Methionine,N-[[5-[[(1H-imidazol-4-ylmethyl)amino]methyl]-2'-methyl[1,1'-biphenyl]-2-yl]carbonyl]-, methyl ester
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| Synonyms |
FTI2153 FTI 2153 FTI-2153
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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 Vitro) |
DMSO : ~90 mg/mL (~192.88 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.36 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 (5.36 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 (5.36 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 | 2.1432 mL | 10.7158 mL | 21.4316 mL | |
| 5 mM | 0.4286 mL | 2.1432 mL | 4.2863 mL | |
| 10 mM | 0.2143 mL | 1.0716 mL | 2.1432 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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