FTI 277 (N-[4-[2(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl]methionine methyl ester trifluoroacetate salt) | 1217447-06-7

name

fti 277

chemical name

n-[4-[2(r)-amino-3-mercaptopropyl]amino-2-phenylbenzoyl]methionine methyl ester trifluoroacetate salt

activity

prodrug form of fti 276 (cat. no. 2406) that inhibits farnesyltransferase (ftase) (ic50 = 0.5 nm). inhibits h-ras and k-ras processing in whole cells (ic50 values are 0.1 and 10 μm respectively) and disrupts constitutive h-ras-specific activation of mapk. causes significant antiproliferative effects in human malignant glioma cells and many other tumor cell lines.

MW

561.64

Formula:

c22h29n3o3s2.c2hf3o2

Solubility:

soluble to 5 mm in water

Purity:

>95 %

Storage:

store at -80°c

CAS No:

1217447-06-7

Lerner et al (1995) Ras CAAX peptidomimetic FTI-277 selectively blocks oncogenic Ras signaling inducing cytoplasic accumulation of inactive Ras-Raf complexes. J.Biol.Chem. 270 26802. PMID: 7592920.

Lerner et al (1995) Disruption of oncogenic K-Ras4B processing and signaling by a potent geranylgeranyltransferase I inhibitor. J.Biol.Chem. 10 26770.

Sun et al (1999) Antitumour 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. 59 4919. PMID: 10519405.