A farnesyltransferase inhibitor with antitumor activity
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Enantiomer(s)
35515(S)-Tipifarnib
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Tipifarnib

Item No. 11747

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[(R)-amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone
CAS Number
192185-72-1
Synonyms
  • R 115777
Molecular Formula
C27H22Cl2N4O
Formula Weight
489.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 10 mg/mlEthanol: 5 mg/ml
λmax
237, 285, 340 nm
SMILES
ClC1=CC=CC(C(C2=C3C=CC([C@@](C4=CC=C(Cl)C=C4)(N)C5=CN=CN5C)=C2)=CC(N3C)=O)=C1
InChi Code
InChI=1S/C27H22Cl2N4O/c1-32-16-31-15-25(32)27(30,18-6-9-20(28)10-7-18)19-8-11-24-23(13-19)22(14-26(34)33(24)2)17-4-3-5-21(29)12-17/h3-16H,30H2,1-2H3/t27-/m1/s1
InChi Key
PLHJCIYEEKOWNM-HHHXNRCGSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Cayman Chemical
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    Product Description

    Tipifarnib is a nonpeptidomimetic, CAAX-competitive inhibitor of farnesyltransferase (IC50 = 0.86 nM).1 It prevents farnesylation of Ras GTPases and has shown potent efficacy in various in vitro and in vivo tumor models.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bell, I.M. Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy? J. Med. Chem. 47(8), 1869-1878 (2004).

    2. Vigil, D., Cherfils, J., Rossman, K.L., et al. Ras superfamily GEFs and GAPs: Validated and tractable targets for cancer therapy? Nat. Rev. Cancer 10(12), 842-857 (2010).

    3. Appels, N.M.G.M., Beijnen, J.H., and Schellens, J.H.M. Development of farnesyl transferase inhibitors: A review. Oncologist 10(8), 565-578 (2005).