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Lonafarnib

Chemical Structure : Lonafarnib

CAS No.: 193275-84-2

Lonafarnib (SCH-66336, Sch 66336, Sch66336)

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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Biological Activity

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.

Physicochemical Properties

M.Wt 638.83
Formula C27H31Br2ClN4O2
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

(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

References

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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