| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
FTI-2153 targets farnesyltransferase (FTase), the enzyme responsible for catalyzing the farnesylation of proteins such as Ras. Farnesylation is a post-translational modification required for the membrane localization and function of Ras proteins, which are key drivers of cell proliferation and survival. By inhibiting FTase with an IC50 of 1.4 nM, FTI-2153 blocks Ras farnesylation and downstream signaling. The compound shows >3000-fold selectivity for inhibition of H-Ras processing over Rap1A processing.
|
|---|---|
| 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]
In vitro, FTI-2153 potently inhibits FTase with an IC50 of 1.4 nM. It effectively inhibits H-Ras protein processing with an IC50 of 10 nM. The compound shows >3000-fold greater potency for H-Ras compared to Rap1A protein processing. This high selectivity makes FTI-2153 a valuable tool for studying Ras-dependent signaling pathways and evaluating FTase as a therapeutic target in cancer. |
| ln Vivo |
In vivo, FTI-2153 has been studied in preclinical cancer models to evaluate the effects of FTase inhibition on tumor growth. By blocking Ras farnesylation and membrane localization, the compound inhibits Ras-mediated signaling and tumor progression. Specific in vivo efficacy data and animal study protocols are available in the primary literature but are not detailed in the available sources.
|
| Enzyme Assay |
Not specifically documented for FTI-2153. For FTase inhibitors, cell-free enzyme assays typically measure the inhibition of farnesyltransferase activity using purified enzyme preparations and farnesyl pyrophosphate (FPP) and peptide substrates. Radiolabeled or fluorescence-based detection methods are used to quantify enzyme activity. IC50 values are determined from concentration-response curves. Selectivity profiling against other prenyltransferases may also be performed.
|
| 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 In vitro cell-based assays for FTI-2153 include assessment of H-Ras processing and membrane localization in Ras-transformed cells. Cell proliferation and survival assays in cancer cell lines with activating Ras mutations can evaluate the effects of FTase inhibition on cell growth. Signaling pathway analysis by Western blot can assess inhibition of downstream Ras effectors such as MAPK and PI3K pathways. |
| Animal Protocol |
In vivo studies with FTI-2153 are conducted in mouse xenograft models of Ras-driven cancers. The compound is typically administered via intraperitoneal or oral routes. Endpoints include tumor growth inhibition, assessment of Ras processing in tumor tissues, and evaluation of downstream signaling. Dosing regimens and specific animal models are detailed in the primary literature.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for FTI-2153 are not extensively documented in the available literature. The compound is a small molecule with molecular weight 466.6 and formula C25H30N4O3S. It has a purity of ≥95%. Detailed PK parameters such as half-life, bioavailability, and clearance have not been reported in the available sources.
|
| Toxicity/Toxicokinetics |
Specific toxicity data for FTI-2153 are not provided in the available literature. As a research compound, it is not intended for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound. The compound is supplied for research purposes only and is not for therapeutic use.
|
| References |
|
| Additional Infomation |
FTI-2153 has the IUPAC name methyl (2S)-2-[[4-[(1H-imidazol-5-ylmethylamino)methyl]-2-(2-methylphenyl)benzoyl]amino]-4-methylsulfanylbutanoate. The molecular formula is C25H30N4O3S with a molecular weight of 466.6. It is a potent and highly selective FTase inhibitor with IC50 of 1.4 nM. The compound is used in cancer research.
|
| Molecular Formula |
C25H30N4O3S
|
|---|---|
| Molecular Weight |
466.595704555511
|
| Exact Mass |
466.204
|
| CAS # |
344900-92-1
|
| Related CAS # |
FTI-2153 TFA;2820151-01-5
|
| PubChem CID |
6918458
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
4.481
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
33
|
| Complexity |
623
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CC1=CC=CC=C1C2=C(C=CC(=C2)CNCC3=CN=CN3)C(=O)N[C@@H](CCSC)C(=O)OC
|
| InChi Key |
KZCMMZOLCBZLNG-QHCPKHFHSA-N
|
| 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
|
| Chemical Name |
L-Methionine,N-[[5-[[(1H-imidazol-4-ylmethyl)amino]methyl]-2'-methyl[1,1'-biphenyl]-2-yl]carbonyl]-, methyl ester
|
| Synonyms |
FTI2153 FTI 2153 FTI-2153
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~90 mg/mL (~192.88 mM)
|
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA