Tipifarnib

Research use only, not for human use.

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

Tipifarnib ((IND 58359, R115777) is a potent and selective inhibitor of FTase (farnesyltransferase); inhibits the farnesylation of lamin B and K-RasB peptide substrates with IC50s of 0.86 nM and 7.9 nM, respectively; no activity for PGGT1(IC50>50 uM); shows sensiticity for tumor cell lines bearing H-ras or N-ras mutations; inhibits the growth of tumors bearing mice and orally bioavailable.Blood Cancer Phase 3 Clinical.

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Animal Model:GalN/LPS challenge mouseDosage:10 mg/kg; while chanllenge with GalN (400 mg/kg; IP) and LPS (32 g/kg) Administration:IP; 60 min before challenge Result:Protected primary hepatocytes from GalN/tumor necrosis factor-induced cell death.Inhibited caspase 3 activation and upregulating antiapoptotic proteins.

IND 58359 | R115777 | IND-58359 | IND58359 | R-115777 | R 115777

Metabolic Enzyme/Protease

Ftase

Farnesyltransferase(FTase)

Cancer

Blood cancer

192185-72-1

489.3958

C27H22Cl2N4O

>98% (HPLC)

10 mM in DMSO

O=C1N(C)C2=C(C=C([C@@](C3=CC=C(Cl)C=C3)(N)C4=CN=CN4C)C=C2)C(C5=CC=CC(Cl)=C5)=C1

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

(-20℃)

With Ice Pack

≥ 2 years