WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406425
CAS#: 251577-09-0 (free base)
Description: FTI-2148 is a potent farnesyltransferase inhibitor with potential antitumor activity. FTI-2148 is highly selective for FTase (IC50, 1.4 nM) over GGTase I (IC50, 1700 nM). FTI-2148 suppressed the growth of the human lung adenocarcinoma A-549 cells in nude mice by 33, 67, and 91% in a dose-dependent manner. Combination therapy of FTI-2148 with either cisplatin, gemcitabine, or Taxol resulted in a greater antitumor efficacy than monotherapy.
MedKoo Cat#: 406425
Name: FTI-2148 free base
CAS#: 251577-09-0 (free base)
Chemical Formula: C24H28N4O3S
Exact Mass: 452.18821
Molecular Weight: 452.573
Elemental Analysis: C, 63.69; H, 6.24; N, 12.38; O, 10.61; S, 7.08
Related CAS #: 817586-01-9 (TFA) 251577-09-0 (free base)
Synonym: FTI2148; FTI 2148; FTI-2148; FTI-2148 TFA; FTI-2148 trfluoroacetic acid salt; FTI-2148 free base
IUPAC/Chemical Name: (5-((((1H-imidazol-4-yl)methyl)amino)methyl)-2'-methyl-[1,1'-biphenyl]-2-carbonyl)-L-methionine
InChi Key: KULAYTGUTXCHSV-QFIPXVFZSA-N
InChi Code: InChI=1S/C24H28N4O3S/c1-16-5-3-4-6-19(16)21-11-17(12-25-13-18-14-26-15-27-18)7-8-20(21)23(29)28-22(24(30)31)9-10-32-2/h3-8,11,14-15,22,25H,9-10,12-13H2,1-2H3,(H,26,27)(H,28,29)(H,30,31)/t22-/m0/s1
SMILES Code: CSCC[C@H](NC(C1=CC=C(C=C1C2=CC=CC=C2C)CNCC3=CNC=N3)=O)C(O)=O
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 452.573 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Kazi A, Xiang S, Yang H, Chen L, Kennedy P, Ayaz M, Fletcher S, Cummings C, Lawrence HR, Beato F, Kang Y, Kim MP, Delitto A, Underwood PW, Fleming JB, Trevino JG, Hamilton AD, Sebti SM. Dual Farnesyl and Geranylgeranyl Transferase Inhibitor Thwarts Mutant KRAS-Driven Patient-Derived Pancreatic Tumors. Clin Cancer Res. 2019 Oct 1;25(19):5984-5996. doi: 10.1158/1078-0432.CCR-18-3399. Epub 2019 Jun 21. PMID: 31227505; PMCID: PMC6774803.
2: Guida WC, Hamilton AD, Crotty JW, Sebti SM. Protein farnesyltransferase: flexible docking studies on inhibitors using computational modeling. J Comput Aided Mol Des. 2005 Dec;19(12):871-85. doi: 10.1007/s10822-005-9030-2. Epub 2006 May 12. PMID: 16607571.
3: Carrico D, Ohkanda J, Kendrick H, Yokoyama K, Blaskovich MA, Bucher CJ, Buckner FS, Van Voorhis WC, Chakrabarti D, Croft SL, Gelb MH, Sebti SM, Hamilton AD. 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. PMID: 15556768.
4: Sun J, Ohkanda J, Coppola D, Yin H, Kothare M, Busciglio B, Hamilton AD, Sebti SM. 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.
5: Sun J, Blaskovich MA, Knowles D, Qian Y, Ohkanda J, Bailey RD, Hamilton AD, Sebti SM. 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.
