FTI-2148
FTI-2148 is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively.
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- No. CAS: 251577-09-0
- Fòrmula: C24H28N4O3S
- Peso molecular:452.57
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Almacenamiento:
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Actividad biológica
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Chemical Information
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Actividad biológica
IC50: 1.4 nM (FT-1); 1.7 μM (GGT-1)[1]
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Cell Line
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Type | Value | Description | References |
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| NIH3T3 | ED50 |
>25 μM
Compound: 22 (FTI-2148)
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Effective dose against murine 3T3 fibroblasts cells
Effective dose against murine 3T3 fibroblasts cells
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[PMID: 14711313] |
| NIH3T3 | ED50 |
0.02 μM
Compound: 22 (FTI-2148)
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Dose required to block Ras farnesylation in mouse 3T3 fibroblasts
Dose required to block Ras farnesylation in mouse 3T3 fibroblasts
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[PMID: 14711313] |
| NIH3T3 | IC50 |
0.2 μM
Compound: 12(FTI-2148)
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Inhibition of mammalian H-Ras processing in NIH 3T3 cells
Inhibition of mammalian H-Ras processing in NIH 3T3 cells
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[PMID: 11277514] |
FTI-2148 (30 μM) inhibits the farnesylation of the exclusively farnesylated protein HDJ2 in all 3 RAS-transformed NIH3T3 cells[1].FTI-2148 is against P. falciparum PFT, Mammalian PFT and Mammalian PGGT-I with IC50 values of 15 nM; 0.82 nM and 1700 nM, respectively. PFT:protein farnesyltransferase; PGGT-I geranylgeranyltransferase-I[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KRAS HRAS, and NRAS-transformed NIH3T3 cells
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Concentration:30 μM
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Incubation Time:
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Result:Inhibited the prenylation of KRAS and NRAS.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Ras transgenic mouse model[3]
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Dosage:100 mg/kg/day
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Administration:Subcutaneous injection; 100 mg/kg/day; 14 days
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Result:Induced regression by 87 ± 3% of mammary carcinomas in mice.
Chemical Information
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No. CAS 251577-09-0
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Peso molecular 452.57
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Fòrmula C24H28N4O3S
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SMILES
CSCC[C@@H](C(O)=O)NC(C1=CC=C(CNCC2=CN=CN2)C=C1C3=CC=CC=C3C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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. [Content Brief]
[2]. Carrico D, et al.In vitro and in vivo antimalarial activity of peptidomimetic protein farnesyltransferase inhibitors with improved membrane permeability.Bioorg Med Chem. 2004 Dec 15;12(24):6517-26. [Content Brief]
[3]. Sun J, et al. Geranylgeranyltransferase I inhibitor GGTI-2154 induces breast carcinoma apoptosis and tumor regression in H-Ras transgenic mice.Cancer Res. 2003 Dec 15;63(24):8922-9. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FTI-2148 Related Classifications
HY-118916 Related Classifications
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