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Submit ReviewFTI 277 is a 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.
分子量 | 561.64 |
公式 | C22H29N3O3S2.C2HF3O2 |
储存 | Store at -80°C |
纯度 | ≥95% (HPLC) |
CAS Number | 1217447-06-7 |
PubChem ID | 71311821 |
InChI Key | GJEFFRDWFVSCOJ-PXPMWPIZSA-N |
Smiles | SC[C@H](N)CNC1=CC=C(C(N[C@H]([C@@](OC)=O)CCSC)=O)C(C2=CC=CC=C2)=C1.FC(F)(C(O)=O)F |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
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
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, Tax. and gemcit. Cancer Res. 59 4919 PMID: 10519405
Lerner et al (1995) Disruption of oncogenic K-Ras4B processing and signaling by a potent geranylgeranyltransferase I inhibitor. J.Biol.Chem. 10 26770
关键词: FTI 277, FTI 277 supplier, Prodrug, FTI, 276, 2406, farnesyltransferase, FTase, H-Ras, K-Ras, MAPK, anti-proliferative, antiproliferative, tumour, tumor, FTI277, Protein, Prenyltransferases, Post-translational, Modifications, 2407, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 FTI 277 的部分引用包括:
Luttman et al (2021) ABL allosteric inhibitors synergize with statins to enhance apoptosis of metastatic lung cancer cells. Cell Rep. 37 109880 PMID: 34706244
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