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G蛋白偶联受体/G蛋白
自噬 代谢酶
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自噬
Transferase Ras
/ Lonafarnib/洛那法尼

Lonafarnib/洛那法尼 {[allProObj[0].p_purity_real_show]}

货号：A257211 同义名： 氯那法尼 / Sch66336; Sarasar

Lonafarnib is a FPTase inhibitor. It can inhibit H-ras (IC50 = 1.9 nM), K-ras-4B (IC50 = 5.2 nM) and N-ras (IC50 = 2.8 nM).

Lonafarnib/洛那法尼 化学结构 CAS号：193275-84-2
Lonafarnib/洛那法尼 化学结构
CAS号：193275-84-2
Lonafarnib/洛那法尼 3D分子结构
CAS号：193275-84-2
Lonafarnib/洛那法尼 化学结构 CAS号：193275-84-2
Lonafarnib/洛那法尼 3D分子结构 CAS号：193275-84-2
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Lonafarnib/洛那法尼 纯度/质量文件 产品仅供科研

货号：A257211 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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PFK-015 ++

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
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Tipifarnib +++

FTase, IC50: 0.6 nM

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Tolcapone +

COMT, Ki: 30 nM

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Lonafarnib +++

K-ras-4B, IC50: 2.8 nM

H-ras, IC50: 1.9 nM

 		99%+
(E)-Daporinad ++++

NMPRTase, Ki: 0.4 nM

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FTI-277 HCl ++++

FTase, IC50: 500 pM

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A 922500 ++

human DGAT-1, IC50: 7 nM

mouse DGAT-1, IC50: 24 nM

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Lomeguatrib ++

O6-alkylguanine-DNA-alkyltransferas, IC50: 5 nM

 		99%+
PF-04620110 +

DGAT1, IC50: 19 nM

 		99%
LB42708 +++

FTase (K-Ras), IC50: 0.8 nM

FTase (N-ras), IC50: 1.2 nM

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GGTI298 Trifluoroacetate ✔ 98%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Lonafarnib/洛那法尼 生物活性

靶点

  • Transferase

    K-ras-4B, IC50:2.8 nM

    H-ras, IC50:1.9 nM
描述 Lonafarnib (Sch66336) effectively disrupts Ha-Ras processing in intact cells and inhibits the abnormal growth characteristics of fibroblasts and human cancer cell lines that carry active Ki-Ras proteins[1]. Groups treated with Lonafarnib (10 μM) exhibited a marked increase in the levels of unfarnesylated H-Ras (116-137%) when compared to those receiving the control treatment[2].

Lonafarnib/洛那法尼 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 数据源
Cos-1 monkey kidney cells Function assay Inhibition of Protein farnesyltransferase in Cos-1 monkey kidney cells expressing H-Ras-val, IC50=0.0019 μM 12190309
COS-7 monkey cells Function assay Inhibiting the farnesylation of H-ras proteins in COS-7 monkey cells transiently expressing H-ras[Val12]-CVLS in the whole cell assay, IC50=0.01 μM 9822558
HCT116 Growth inhibition assay Compound was measured for inhibition of HCT116 tumor cell line in colon under soft agar assay, IC50=0.07 μM 9822558
MCF-7 tumor cell line Growth inhibition assay Compound was measured for inhibition of MCF-7 tumor cell line in breast under soft agar assay, IC50=0.05 μM 9822558

Lonafarnib/洛那法尼 动物研究

Animal study Lonafarnib (Sch66336) showcases exceptional oral bioavailability and pharmacokinetic profiles across mouse, rat, and monkey models. In studies using nude mice, Lonafarnib has shown significant efficacy when administered orally against a variety of human cancer xenografts, including those from the colon, lung, pancreas, prostate, and bladder[1].Administered alone at a dosage of 80 mg/kg orally once a day, Lonafarnib shows a modest capacity to suppress the growth of orthotopic U87 tumors, with a therapeutic/control ratio (T/C) of 0.67, when compared to animals treated with the control vehicle. The regimen of XRT/Tem, involving 2.5Gy of radiation therapy per day for two days coupled with Temozolomide at 5 mg/kg given orally 90 minutes before radiation, is engineered to achieve a moderate level of tumor growth inhibition in vivo, demonstrating a T/C ratio of 0.42. A combined treatment involving Lonafarnib, given at 80 mg/kg orally once daily, radiation therapy at 2.5Gy per day for two days, and Temozolomide at 5 mg/kg orally 90 minutes before radiation, results in the most significant reduction of tumor growth (T/C of 0.02). This combination is substantially more effective than just XRT/Tem (p<0.04), with a majority of the subjects showing a reduction in tumor volume after two weeks, a result that remains after four weeks (p<0.05)[2].

Lonafarnib/洛那法尼 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00040534 Neoplasms Phase 1 Terminated - -
NCT00040547 Neoplasms Phase 1 Completed - -
NCT00003956 Lymphoma Unsp... 展开 >>ecified Adult Solid Tumor, Protocol Specific 收起 << Phase 1 Completed - United States, New York ... 展开 >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 收起 <<

Lonafarnib/洛那法尼 参考文献

[1]Liu M, et al. Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice. Cancer Res. 1998 Nov 1;58(21):4947-56.

[2]Chaponis D, et al. Lonafarnib (SCH66336) improves the activity of temozolomide and radiation for orthotopic malignant gliomas. J Neurooncol. 2011 Aug;104(1):179-89.

[3]Bailey TJ, et al. The inhibitor of phagocytosis, O-phospho-L-serine, suppresses Müller glia proliferation and cone cell regeneration in the light-damaged zebrafish retina. Exp Eye Res. 2010 Nov;91(5):601-12.

Lonafarnib/洛那法尼 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.57mL

0.31mL

0.16mL

7.83mL

1.57mL

0.78mL

15.65mL

3.13mL

1.57mL

Lonafarnib/洛那法尼 技术信息

CAS号193275-84-2
分子式C27H31Br2ClN4O2
分子量 638.82
SMILES Code O=C(N1CCC(CC(N2CCC([C@@H]3C4=C(Br)C=C(Cl)C=C4CCC5=CC(Br)=CN=C53)CC2)=O)CC1)N
MDL No. MFCD06795138
别名 氯那法尼 ;Sch66336; Sarasar
运输蓝冰
InChI Key DHMTURDWPRKSOA-RUZDIDTESA-N
Pubchem ID 148195
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二

Tags: Lonafarnib | 193275-84-2 | Sch66336 | Sch 66336 | Sch-66336 | FPTase Inhibitor | Metabolic Enzyme/Protease | MAPK/ERK Pathway | GPCR/G Protein | Autophagy | Farnesyl Transferase | Ras | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Lonafarnib/洛那法尼 纯度/质量文件 | Lonafarnib/洛那法尼 亚型比较 | Lonafarnib/洛那法尼 生物活性 | Lonafarnib/洛那法尼 细胞研究 | Lonafarnib/洛那法尼 动物研究 | Lonafarnib/洛那法尼 临床数据 | Lonafarnib/洛那法尼 参考文献 | Lonafarnib/洛那法尼 实验方案 | Lonafarnib/洛那法尼 技术信息

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