Tipifarnib, Free base | 2296

A potent, selective, nonpeptidomimetic inhibitor of farnesyl protein transferase (FPT), an enzyme involved in protein processing (farnesylation) for signal transduction. Displays significant antitumor effects in vivo. Tipifarnib competitively inhibits the farnesylation of lamin B (IC₅₀ = 0.86 nM) and K-RasB (IC₅₀ = 7.9 nM) peptide substrates and inhibits the cell growth of ~75% of a panel of 53 human tumor cell lines tested.

Tipifarnib is a potent, selective, nonpeptidomimetic inhibitor of farnesyl protein transferase (FPT), an enzyme involved in protein processing (farnesylation) for signal transduction

2296 | Tipifarnib, Free base DataSheet

Alternate Name/Synonyms: (R)-6-(Amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl)-4-(3-chlorophenyl)-1-methylquinolin-2(1H)-one; R-115777

Appearance: White to off-white solid

Formulation: N/A

CAS Number: 192185-72-1

Structure Available?: Yes

Peptide sequence: No

Salt Form: No

Molecular Formula: C₂₇H₂₂Cl₂N₄O

Molecular Weight: 489.4

Cell-Permeable?: Yes

Purity: ≥98% by HPLC

Solubilities: DMSO (~ 15 mg/ml) or Ethanol (~ 10 mg/ml)

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A potent farnesyl protein transferase (FPT) inhibitor

MDL Number: MFCD09837802

PubChem CID: 159324

SMILES: CN1C=NC=C1C(C2=CC=C(C=C2)Cl)(C3=CC4=C(C=C3)N(C(=O)C=C4C5=CC(=CC=C5)Cl)C)N

InChi: 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