FTI-276 is a potent and selective farnesyltransferase inhibitor, which is also a tetrapeptide mimetic of the carboxyl terminus of K-Ras4B. FTI-276 blocked the growth in nude mice of a human lung carcinoma that expresses the two most prevalent genetic alterations in human cancers (K-Ras oncogenic mutation and deletion in the tumor suppressor gene p53). In contrast, FTI-276 did not inhibit tumor growth of a human lung carcinoma that harbors no Ras mutations. Furthermore, FTI-276 inhibited oncogenic signaling and tumor growth of NIH 3T3 cells transformed with the ras but not the raf oncogene.
CAS 170006-72-1 MFCD06409253
化学结构图
SMILES: CSCC[C@H](NC(=O)c1ccc(NC[C@@H](N)CS)cc1-c1ccccc1)C(=O)O
化学属性
| Mol. Formula | C21H27N3O3S2·C2HF3O2 |
|---|---|
| Mol. Weight | 433.59 |
| Appearance | Solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | FTI-276 is a potent and selective farnesyltransferase inhibitor, which is also a tetrapeptide mimetic of the carboxyl terminus of K-Ras4B. FTI-276 blocked the growth in nude mice of a human lung carcinoma that expresses the two most prevalent genetic alterations in human cancers (K-Ras oncogenic mutation and deletion in the tumor suppressor gene p53). In contrast, FTI-276 did not inhibit tumor growth of a human lung carcinoma that harbors no Ras mutations. Furthermore, FTI-276 inhibited oncogenic signaling and tumor growth of NIH 3T3 cells transformed with the ras but not the raf oncogene. |
|---|---|
| Synonym | FTI276; FTI-276; FTI 276. N-[4-[2-(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl]methionine trifluoroacetate salt |
| CAS Number | 170006-72-1 (free base) |
| MDL Number | MFCD06409253 |
| PubChem Substance ID | 329799788 |
| Formula | C21H27N3O3S2 |
| IUPAC Name | (S)-2-(5-(((R)-2-amino-3-mercaptopropyl)amino)-[1,1'-biphenyl]-2-ylcarboxamido)-4-(methylthio)butanoic acid. |
| InChIKey | ZIXDDEATQSBHHL-BEFAXECRSA-N |
| InChI | InChI=1S/C21H27N3O3S2/c1-29-10-9-19(21(26)27)24-20(25)17-8-7-16(23-12-15(22)13-28)11-18(17)14-5-3-2-4-6-14/h2-8,11,15,19,23,28H,9-10,12-13,22H2,1H3,(H,24,25)(H,26,27)/t15-,19+/m1/s1 |
| Canonical SMILES | CSCC[C@@H](C(O)=O)NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=CC=CC=C2)=O |
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分类
- {SNA} Bioactive Small Molecule Alphabetical Index,
- {SNA} Bioactive Small Molecules, Biochemicals and Reagents, Cell Biology, Cell Signaling and Neuroscience, D to K, Enzyme Inhibitors, Enzyme Inhibitors by Enzyme, Enzymes, Inhibitors, and Substrates, F, Farnesyl transferase, G Protein Function,
- {
- Bioactive Small Molecules,
产品应用
- FTI-276 is a potent and selective farnesyltransferase inhibitor, which is also a tetrapeptide mimetic of the carboxyl terminus of K-Ras4B. FTI-276 blocked the growth in nude mice of a human lung carcinoma that expresses the two most prevalent genetic alterations in human cancers (K-Ras oncogenic mutation and deletion in the tumor suppressor gene p53). In contrast, FTI-276 did not inhibit tumor growth of a human lung carcinoma that harbors no Ras mutations. Furthermore, FTI-276 inhibited oncogenic signaling and tumor growth of NIH 3T3 cells transformed with the ras but not the raf oncogene.
相关文献及参考
- Cohen-Johnson, E., et al., The farnesyltransferase inhibitor FTI-277 suppresses the 24-kDa FGF2-induced radioresistance in HeLa cells expressing wild-type RAS. Radiat. Res. 152 , 404-411, (1999) 摘要
- [1]. Chakrabarti D, et al. Protein farnesyltransferase and protein prenylation in Plasmodium falciparum.J Biol Chem. 2002 Nov 1; 277(44):42066-73. Epub 2002 Aug 22.
安全信息
GHS Symbol
- H315 Causes skin irritation 会刺激皮肤
- H319 Causes serious eye irritation 严重刺激眼睛
- H335 May cause respiratory irritation 可能导致呼吸道刺激
- P261 Avoid breathing dust/fume/gas/mist/vapours/spray. 避免吸入粉尘/烟/气体/烟雾/蒸汽/喷雾。
- P305+P351+P338
- S26 In case of contact with eyes, rinse immediately with plenty of water and seek medical advice 眼睛接触后，立即用大量水冲洗并征求医生意见；
- S36 Wear suitable protective clothing 穿戴适当的防护服；
- R36/37/38 Irritating to eyes, respiratory system and skin 对眼睛、呼吸系统和皮肤有刺激性
