≥98% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
FTI-2153 is a potent and highly selective inhibitor of farnesyltransferase (FTase) , with an IC 50 of 1.4 nM. FTI-2153 is >3000-fold more potent at blocking H-Ras ( IC 50 , 10 nM) than Rap1A processing. Anti-cancer activity.
In Vitro
FTI-2153, inhibits bipolar spindle formation during mitosis independently of transformation and Ras and p53 mutation status in two human lung cancer cell lines. FTI-2153 increases the percentage of prometaphase cells with ring-like DNA morphology in transformed and non-transformed cells. FTI-2153 (15 μM) inhibits T-24 and Calu-1 cell growth by 38 and 36%, respectively. NIH3T3, HFF and HT-1080 are less sensitive and are inhibited by only 8, 8 and 13%, respectively. A-549 and OVCAR3 cell growth is inhibited by 25 and 22%, respectively. Thus, even though T-24 and Calu-1 cells are equisensitive to FTI-2153 cell growth inhibition, FTI-2153 inhibits bipolar spindle formation only in Calu-1 cells. HFF and NIH3T3 cells are both resistant to FTI2153 growth inhibition, yet only NIH3T3 cells are resistant to FTI-2153 inhibition of bipolar spindle formation. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: NIH3T3, HFF, HT1080, T-24, OVCAR3, A-549 and Calu-1 CELLS. Concentration: 48 h. Incubation Time: 15 μM. Result: When A-549 cells were treated with FTI-2153 (15 μM for 48 h), the proportion of cells at prometaphase increased relative to the other phases of mitosis. FTI-2153 accumulated cells at prometaphase with a rosette-like morphology where chromosomes form a ring surrounding a monoaster of microtubules. In all cells, except for T-24 and NIH3T3, FTI-2153 treatment increased the proportion of mitotic cells in prometaphase and decreased the percentage of cells in telophase/cytokinesis. In HT1080 cells, the percentage of cells in prometaphase and telophase/ cytokinesis were 5 and 85% in control cells and 55 and 35% in Treated cells, respectively. Similarly results were also found in HFF cells. Calu-1 and A-549 cells, as described previously, had similarly large changes, whereas OVCAR3 had smaller changes. In contrast, FTI-2153 did not significantly affect the distribution of the different phases of mitosis in T-24 and NIH3T3 cells.
Form:Solid
| Isomères SMILES | CC1=CC=CC=C1C2=C(C=CC(=C2)CNCC3=CN=CN3)C(=O)N[C@@H](CCSC)C(=O)OC |
|---|---|
| PubChem CID | 6918458 |
| Poids moléculaire | 466.60 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Solubilité | DMSO : 100 mg/mL (214.32 mM; Need ultrasonic) |
|---|---|
| Poids moléculaire | 466.600 g/mol |
| XLogP3 | 3.200 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 6 |
| Rotatable Bond Count | 12 |
| Exact Mass | 466.204 Da |
| Monoisotopic Mass | 466.204 Da |
| Topological Polar Surface Area | 121.000 Ų |
| Heavy Atom Count | 33 |
| Formal Charge | 0 |
| Complexity | 622.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 1 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
