A peptidomimetic inhibitor of FTase
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FTI-276 (trifluoroacetate salt)

Item No. 10011661

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[[5-[[(2R)-2-amino-3-mercaptopropyl]amino][1,1′-biphenyl]-2-yl]carbonyl]-L-methionine, 2,2,2-trifluoroacetate
CAS Number
1217471-51-6
Synonyms
  • Farnesyltransferase Inhibitor 276
Molecular Formula
C21H27N3O3S2 • CF3COOH
Formula Weight
547.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Water: 10 mM
SMILES
O=C(N[C@H](C(O)=O)CCSC)C1=CC=C(NC[C@@H](N)CS)C=C1C2=CC=CC=C2.OC(C(F)(F)F)=O
InChi Code
InChI=1S/C21H27N3O3S2.C2HF3O2/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;3-2(4,5)1(6)7/h2-8,11,15,19,23,28H,9-10,12-13,22H2,1H3,(H,24,25)(H,26,27);(H,6,7)/t15-,19+;/m1./s1
InChi Key
IAVHISGQCODLHL-WSCVZUBPSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    Product Description

    FTI-276 is a CAAX peptidomimetic inhibitor of farnesyltransferase (FTase; IC50 = 500 pM).1 It contains the C-terminal CAAX sequence, Cys-Val-Iso-Met (CVIM), of K-Ras4B, a form of Ras that is commonly mutated in human cancers, and is selective for FTase over geranylgeranyltransferase I (GGTase I; IC50 = 50 nM). It inhibits the growth of NIH3T3 cells expressing oncogenic farnesylated H-Ras (RasF), but not geranylgeranylated H-Ras (RasGG) or Raf, when used at a concentration of 20 µM.2 FTI-276 (50 mg/kg) also reduces tumor growth in a mouse xenograft model using Calu-1 cells that contain a K-Ras oncogenic mutation but not in a model using NCI H810 cells that do not contain a K-Ras mutation.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lerner, E.C., Qian, Y., Blaskovich, M.A., et al. Ras CAAX peptidomimetic FTI-277 selectively blocks oncogenic Ras signaling by inducing cytoplasmic accumulation of inactive Ras-Raf complexes. The Journal of Biological Chemisty 270(45), 26802-26806 (1995).

    2. Sun, J., Qian, Y., Hamilton, A.D., et al. Ras CAAX peptidomimetic FTI 276 selectively blocks tumor growth in nude mice of a human lung carcinoma with K-Ras mutation and p53 deletion. Cancer Res. 55(19), 4243-4247 (1995).