Chemical Structure : Lonafarnib
CAS No.: 193275-84-2
Catalog No.: PC-21769Not For Human Use, Lab Use Only.
Lonafarnib (SCH 66336) is a potent, orally bioavailable farnesyl protein transferase (FTase, farnesyltransferase) inhibitor with IC50 of 1.9 nM for H-Ras processing in whole cells.
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Lonafarnib (SCH 66336) is a potent, orally bioavailable farnesyl protein transferase (FTase, farnesyltransferase) inhibitor with IC50 of 1.9 nM for H-Ras processing in whole cells.
Lonafarnib (SCH 66336) inhibits K-ras and N-ras with IC50 of 5.2 nM and 2.8 nM, respectively. blocks the trans formed growth properties of fibroblasts and human tumor cell lines expressing activated Ki-Ras proteins.
Lonafarnib (SCH 66336) inhibits tumor growth in nude mice treated with cells that contained either K-ras mutations (MIA PACA-2, human pancreatic cancer, and HCT-116, human colon cancer) or H-ras mutations (transformed mouse fibroblast, NIH3T3-CVLS), in a dose-dependent manner.
Lonafarnib (SCH 66336) exhibits good oral pharmacokinetics in monkeys and showed good oral efficacy as an antitumor agent in mice.
M.Wt | 638.83 | |
Formula | C27H31Br2ClN4O2 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
(R)-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 |
1. Liu M, et al. Cancer Res. 1998 Nov 1;58(21):4947-56.
2. Njoroge FG, et al. J Med Chem. 1998 Nov 19;41(24):4890-902.
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