| Identification | Back Directory | [Name]
FTI-2148 | [CAS]
251577-09-0 | [Synonyms]
FTI-2148
N-[5-(1H-Imidazol-4-ylmethylaminomethyl)-2'-methylbiphenyl-2-ylcarbonyl]-L-methionine
L-Methionine, N-[[5-[[(1H-imidazol-5-ylmethyl)amino]methyl]-2'-methyl[1,1'-biphenyl]-2-yl]carbonyl]- | [Molecular Formula]
C24H28N4O3S | [MDL Number]
MFCD08056245 | [MOL File]
251577-09-0.mol | [Molecular Weight]
452.57 |
| Chemical Properties | Back Directory | [Boiling point ]
730.1±60.0 °C(Predicted) | [density ]
1.256±0.06 g/cm3(Predicted) | [solubility ]
DMSO:0.0(Max Conc. mg/mL);0.0(Max Conc. mM) | [pka]
3.49±0.10(Predicted) |
| Hazard Information | Back Directory | [Uses]
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[1]. | [in vivo]
FTI-2148 (intraperitoneal injection; 25 or 50 mpk/day with a mini-pump; started on day 15 and stopped on day 45 and restarted day 53-83) inhibits the tumor growth by 91% in human lung adenocarcinoma A-549 cells induced mouse model[1].
FTI-2148 (subcutaneous injection; 25 mpk/day with a mini-pump; 14 days) inhibits tumor growth by 77%by the end of the 2-week treatment in Human Xenograft Nude Mouse Model[1].FTI-2148 (subcutaneous injection; 100 mg/kg/day; 14 days) results in breast tumor regression in a ras transgenic mouse model[1].
FTI-2148 (subcutaneous injection; 100 mg/kg/day; 4 days) results in 85-88% inhibition of FTase with no inhibition of GGTase I enzymatic activity in breast tumors from mice in vivo settings[3]. | Animal Model: | Ras?transgenic mouse model[3] | | Dosage: | 100 mg/kg/day | | Administration: | Subcutaneous?injection; 100 mg/kg/day; 14 days | | Result: | Induced regression by 87 ± 3% of mammary carcinomas in mice. |
| [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. PMID:10519405
[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. DOI:10.1016/j.bmc.2004.09.020
[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. PMID:14695209 |
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| Company Name: |
InvivoChem
|
| Telephone: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|