FTI-277 HCl

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406300

CAS#: 180977-34-8 (HCl)

Description: FTI-277 is a peptide mimetic of the COOH-terminal Cys-Val-Ile-Met of K-Ras4B that inhibited potently FTase in vitro (IC50 = 500 pM) and was highly selective for FTase over geranylgeranyltransferase I (GGTase I) (IC50 = 50 nM). FTI-277, the methyl ester derivative of FTI-276, was extremely potent (IC50 = 100 nM) at inhibiting H-Ras, but not the geranylgeranylated Rap1A processing in whole cells.

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FTI-277-HCl is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.

Chemical Structure


Theoretical Analysis

MedKoo Cat#: 406300
Name: FTI-277 HCl
CAS#: 180977-34-8 (HCl)
Chemical Formula: C22H30ClN3O3S2
Exact Mass:
Molecular Weight: 484.07
Elemental Analysis: C, 54.59; H, 6.25; Cl, 7.32; N, 8.68; O, 9.92; S, 13.25

Related CAS #: 170006-73-2 (free base)   180977-34-8 (HCl)   1217447-06-7 (TFA)    

Synonym: FTI-277; FTI 277; FTI277; FTI-227 hydrochloride, FTI-227 HCl.

IUPAC/Chemical Name: methyl (5-(((R)-2-amino-3-mercaptopropyl)amino)-[1,1'-biphenyl]-2-carbonyl)-L-methioninate hydrochloride


InChi Code: InChI=1S/C22H29N3O3S2.ClH/c1-28-22(27)20(10-11-30-2)25-21(26)18-9-8-17(24-13-16(23)14-29)12-19(18)15-6-4-3-5-7-15;/h3-9,12,16,20,24,29H,10-11,13-14,23H2,1-2H3,(H,25,26);1H/t16-,20+;/m1./s1


Technical Data

Solid powder

>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).

Soluble in DMSO and 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).

Harmonized System Code:

Additional Information

Treatment of H-Ras oncogene-transformed NIH 3T3 cells with FTI-277 blocked recruitment to the plasma membrane and subsequent activation of the serine/threonine kinase c-Raf-1 in cells transformed by farnesylated Ras (H-RasF), but not geranylgeranylated, Ras (H-RasGG). FTI-277 induced accumulation of cytoplasmic non-farnesylated H-Ras that was able to bind Raf and form cytoplasmic Ras/Raf complexes in which Raf kinase was not activated. Furthermore, FTI-277 blocked constitutive activation of mitogen-activated protein kinase (MAPK) in H-RasF, but not H-RasGG, or Raf-transformed cells. FTI-277 also inhibited oncogenic K-Ras4B processing and constitutive activation of MAPK, but the concentrations required were 100-fold higher than those needed for H-Ras inhibition. The results demonstrate that FTI-277 blocks Ras oncogenic signaling by accumulating inactive Ras/Raf complexes in the cytoplasm, hence preventing constitutive activation of the MAPK cascade.


1: Yang W, Yamada M, Tamura Y, Chang K, Mao J, Zou L, Feng Y, Kida K, Scherrer-Crosbie M, Chao W, Ichinose F, Yu YM, Fischman AJ, Tompkins RG, Yao S, Kaneki M. Farnesyltransferase inhibitor FTI-277 reduces mortality of septic mice along with improved bacterial clearance. J Pharmacol Exp Ther. 2011 Dec;339(3):832-41. doi: 10.1124/jpet.111.183558. Epub 2011 Aug 26. PubMed PMID: 21873557; PubMed Central PMCID: PMC3226365.

2: Kim DM, Ryu SW, Choi C. Long-term treatment of farnesyltransferase inhibitor FTI-277 induces neurotoxicity of hippocampal neurons from rat embryo in a ROS-dependent manner. Biochem Biophys Res Commun. 2010 Dec 3;403(1):91-6. doi: 10.1016/j.bbrc.2010.10.123. Epub 2010 Oct 30. PubMed PMID: 21040708.

3: Doisneau-Sixou SF, Cestac P, Faye JC, Favre G, Sutherland RL. Additive effects of tamoxifen and the farnesyl transferase inhibitor FTI-277 on inhibition of MCF-7 breast cancer cell-cycle progression. Int J Cancer. 2003 Sep 20;106(5):789-98. PubMed PMID: 12866041.

4: Girgert R, Wittrock J, Pfister S, Schweizer P. Farnesyltransferase inhibitor FTI-277 prevents autocrine growth stimulation of neuroblastoma by BDNF. J Cancer Res Clin Oncol. 2003 Apr;129(4):227-33. Epub 2003 Apr 17. PubMed PMID: 12700894.

5: Ellis CA, Vos MD, Wickline M, Riley C, Vallecorsa T, Telford WG, Zujewskil J, Clark GJ. Tamoxifen and the farnesyl transferase inhibitor FTI-277 synergize to inhibit growth in estrogen receptor-positive breast tumor cell lines. Breast Cancer Res Treat. 2003 Mar;78(1):59-67. PubMed PMID: 12611458.

6: Bolick SC, Landowski TH, Boulware D, Oshiro MM, Ohkanda J, Hamilton AD, Sebti SM, Dalton WS. The farnesyl transferase inhibitor, FTI-277, inhibits growth and induces apoptosis in drug-resistant myeloma tumor cells. Leukemia. 2003 Feb;17(2):451-7. PubMed PMID: 12592346.

7: Mazzocca A, Giusti S, Hamilton AD, Sebti SM, Pantaleo P, Carloni V. Growth inhibition by the farnesyltransferase inhibitor FTI-277 involves Bcl-2 expression and defective association with Raf-1 in liver cancer cell lines. Mol Pharmacol. 2003 Jan;63(1):159-66. PubMed PMID: 12488548.

8: Nam JS, Ino Y, Sakamoto M, Hirohashi S. Ras farnesylation inhibitor FTI-277 restores the E-cadherin/catenin cell adhesion system in human cancer cells and reduces cancer metastasis. Jpn J Cancer Res. 2002 Sep;93(9):1020-8. PubMed PMID: 12359056.

9: Cohen-Jonathan E, Toulas C, Ader I, Monteil S, Allal C, Bonnet J, Hamilton AD, Sebti SM, Daly-Schveitzer N, Favre G. The farnesyltransferase inhibitor FTI-277 suppresses the 24-kDa FGF2-induced radioresistance in HeLa cells expressing wild-type RAS. Radiat Res. 1999 Oct;152(4):404-11. PubMed PMID: 10477917.

10: Miquel K, Pradines A, Sun J, Qian Y, Hamilton AD, Sebti SM, Favre G. GGTI-298 induces G0-G1 block and apoptosis whereas FTI-277 causes G2-M enrichment in A549 cells. Cancer Res. 1997 May 15;57(10):1846-50. PubMed PMID: 9157972.