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Tipifarnib

Chemical Structure : Tipifarnib

CAS No.: 192185-72-1

Tipifarnib (IND 58359;R115777;IND-58359;IND58359;R-115777;R 115777)

Catalog No.: PC-42624Not For Human Use, Lab Use Only.

Tipifarnib ((IND 58359, R115777) is a potent and selective inhibitor of FTase (farnesyltransferase) with IC50 of 0.86 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Tipifarnib ((IND 58359, R115777) is a potent and selective inhibitor of FTase (farnesyltransferase) with IC50 of 0.86 nM.
Tipifarnib inhibits the farnesylation of lamin B and K-RasB peptide substrates with IC50s of 0.86 nM and 7.9 nM, respectively.
Tipifarnib shows no activity for PGGT1(IC50>50 uM).
Tipifarnib shows sensiticity for tumor cell lines bearing H-ras or N-ras mutations.
Tipifarnib inhibits the growth of tumors bearing mice and orally bioavailable.

Physicochemical Properties

M.Wt 489.3958
Formula C27H22Cl2N4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2(1H)-Quinolinone, 6-[(R)-amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methyl-

References

1. End DW, et al. Cancer Res. 2001 Jan 1;61(1):131-7.

2. Kelland LR, et al. Clin Cancer Res. 2001 Nov;7(11):3544-50.

3. Beaupre DM, et al. Mol Cancer Ther. 2004 Feb;3(2):179-86.

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