LONAFARNIB
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LONAFARNIB ??
- ???
- 214.5-215.9° (monohydrate); mp 222-223°
- ??
- D25 = +49.1° (c = 0.21 in methanol)
- ?? ?
- 710.4±70.0 °C(Predicted)
- ??
- 1.536
- ?? ??
- -20°C
- ???
- ?????(?? ???), ???(?? ???)
- ?? ?? (pKa)
- 15.76±0.40(Predicted)
- ??? ??
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- ?? ? ???? ?? (GHS)
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LONAFARNIB C??? ??, ??, ??
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Lonafarnib is an orally bioavailable tricyclic inhibitor of farnesyl protein transferase. It inhibits Rheb farnesylation and mTOR signaling and enhances taxane and tamoxifen antitumor activity. Studies show that it induces CCAAT/enhancer-binding protein homologous protein-dependent expression of death receptor 5, leading to induction of apoptosis in human cancer cells??
ChEBI: A 4-{2-[4-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl]-2-oxoethyl}piperidine-1-carboxamide that has R configuration. It is used as oral farnesyltransferase nhibitor.?? ??
Lonafarnib (SCH66336) is a farnesyl transferase inhibitor (FTI). K- and N-Ras are substrates of farnesyl transferase.Mechanism of action
Lonafarnib is a protein farnesyltransferase inhibitor (FTI) that reversibly binds to the farnesyltransferase CAAX binding site9, thereby inhibiting progerin farnesylation and subsequent intercalation into the nuclear membrane.???
- vomiting
- diarrhea
- nausea
- stomach pain
- constipation
- gas
- decreased appetite
- decreased weight
LONAFARNIB ?? ?? ? ???
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LONAFARNIB ?? ??
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