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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Farnesyl transferase (FTase)-Lonafarnib
Lonafarnib

Chemical Structure : Lonafarnib

CAS No.: 193275-84-2

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Lonafarnib (SCH-66336, Sch 66336, Sch66336)

货号: 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.

规格 价格 库存 数量
5 mg ￥980 In stock
10 mg ￥1480 In stock
25 mg ￥2580 In stock
50 mg ￥4280 In stock
100 mg ￥6780 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 638.83
分子式 C27H31Br2ClN4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
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

参考文献

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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