FTI-2148 diTFA
- CAS No.
- 817586-01-9
- Chemical Name:
- FTI-2148 diTFA
- Synonyms
- FTI-2148 diTFA
- CBNumber:
- CB08054407
- Molecular Formula:
- C26H29F3N4O5S
- Molecular Weight:
- 566.6
- MDL Number:
- MFCD34469987
- MOL File:
- 817586-01-9.mol
- MSDS File:
- SDS
FTI-2148 diTFA Chemical Properties, Uses, Production
Uses
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[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[3]. 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: | Rastransgenic mouse model[3] |
| Dosage: | 100 mg/kg/day |
| Administration: | Subcutaneousinjection; 100 mg/kg/day; 14 days |
| Result: | Reduced 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] 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
FTI-2148 diTFA Preparation Products And Raw materials
Raw materials
Preparation Products
FTI-2148 diTFA Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 | marketing@targetmol.com | United States | 32431 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 29874 | 58 |
| Supplier | Advantage |
|---|---|
| TargetMol Chemicals Inc. | 58 |
| TargetMol Chemicals Inc. | 58 |
