FTI-2148 diTFA
FTI-2148 diTFA 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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- CAS No.: 817586-01-9
- Formule: C28H30F6N4O7S
- Masse moléculaire:680.62
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
IC50: 1.4 nM (FT-1); 1.7 μM (GGT-1)[1]
FTI-2148 (30 μM) inhibits the farnesylation of the exclusively farnesylated protein HDJ2 in all 3 RAS-transformed NIH3T3 cells[1]. FTI-2148 diTFA 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:Reduced regression by 87 ± 3% of mammary carcinomas in mice.
Chemical Information
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CAS No. 817586-01-9
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Masse moléculaire 680.62
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Formule C28H30F6N4O7S
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SMILES
CSCC[C@@H](C(O)=O)NC(C1=CC=C(CNCC2=CNC=N2)C=C1C3=CC=CC=C3C)=O.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]. 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 diTFA Related Classifications
HY-118916A Related Classifications
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