Lonafarnib (SCH66336)
Lonafarnib (SCH66336) 是一种口服生物有效的FPTase抑制剂，作用于H-ras，K-ras-4B和N-ras，无细胞试验中IC50分别为1.9 nM， 5.2 nM和2.8 nM。Phase 3。
Lonafarnib (SCH66336) Chemical Structure
CAS: 193275-84-2
产品质控
批次：
纯度：
99.48%
99.48
Lonafarnib (SCH66336)相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| Caco-2 | Cytotoxicity assay | 48 hours | Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging, IC50 = 5.68 μM. | ChEMBL | |
| Caco-2 | Toxicity assay | 48 hours | Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay, CC50 = 10.71 μM. | ChEMBL | |
| NIH-H tumor cell lines | Growth inhibition assay | Compound ability to inhibit anchorage-independent growth of NIH-H tumor cell lines in soft agar, IC50=0.072 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 | ||
| 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 | ||
| 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 | ||
| NIH3T3 cells | Function assay | Inhibition of Ras farnesylation in H-Ras transformed NIH3T3 cells, EC50=0.1 μM | 15454228 | ||
| NIH-K tumor cell lines | Growth inhibition assay | Compound ability to inhibit anchorage-independent growth of NIH-K tumor cell lines in soft agar, IC50=0.5 μM | 9822558 | ||
| Cos-1 | Function assay | Inhibition of Protein farnesyltransferase in Cos-1 monkey kidney cells expressing H-Ras-val, IC50 = 0.0019 μM. | 12190309 | ||
| Cos-1 | Function assay | Effect on Ras processing in Cos-1 monkey kidney cells expressing either H-Ras-Val 12-CVLS or H-Ras-Val12, IC50 = 0.01 μM. | 10411485 | ||
| COS7 | Function assay | Inhibition of FTase in human COS7 cells, IC50 = 0.01 μM. | 20925433 | ||
| H-Ras transformed cells | Function assay | Inhibition of soft agar colony formation in H-Ras transformed cells, IC50 = 0.07 μM. | 15501065 | ||
| NIH3T3 | Function assay | Effective concentration against Ha-RAS processing in NIH3T3 ras-transformed cells, EC50 = 0.16 μM. | 12657284 | ||
| NIH3T3 | Function assay | TP_TRANSPORTER: inhibition of DNR efflux (DNR: ? uM) in MDR1-expressing NIH3T3 cells, IC50 = 2.7 μM. | 11606389 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Lonafarnib (SCH66336) 是一种口服生物有效的FPTase抑制剂，作用于H-ras，K-ras-4B和N-ras，无细胞试验中IC50分别为1.9 nM， 5.2 nM和2.8 nM。Phase 3。 | ||||||
|---|---|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | SCH66336在0.1 μM到8 μM浓度范围均可抑制头部和颈部鳞状细胞癌(HNSCC) 生长和诱导凋亡，抑制效果具有剂量和时间依赖性。SCH66336 (8 μM)可在SqCC/Y1细胞中抑制蛋白激酶B/Akt活性和磷酸化 Akt蛋白底物糖原合酶激酶（GSK）- 3β，转录叉因子和BAD[2]。SCH66336 对多细胞系有抗增殖作用，IC 50范围从0.6 μM 到32.3 μM [3] ; Lonafarnib诱导CCAAT /增强子结合蛋白同源蛋白（CHOP）依赖性DR5启动子的转录激活，从而诱导CHOP依赖性的DR5上调。Lonafarnib (< 10 μM) 可激活caspase - 8及其下游的半胱氨酸蛋白酶，从而诱导H1792细胞凋亡。Lonafarnib (5 μM)可增加DR5的细胞表面分布，增强肿瘤坏死因子相关凋亡诱导配体诱导的H1792细胞凋亡[4]。 | |||
|---|---|---|---|---|
| 细胞实验 | 细胞系 | UMSCC10B, UMSCC14B, UMSCC17B, UMSCC22B, 和UMSCC35, UMSCC38 细胞 | ||
| 浓度 | 0.1 μM - 8 μM | |||
| 孵育时间 | 24 小时 | |||
| 方法 | 细胞铺板于96孔板中，后续培养5天，据此确定起始密度。24小时后，用不同浓度SCH66336处理细胞。SCH66336溶解于DMSO。对照组细胞用同样量的DMSO处理。5天后用SRB法检测细胞数量。生长抑制的百分比的计算公式为：增长抑制百分比=（1−/At/Ac）×100，At和Ac分别代表实验组和对照组的吸收值。IC 50值由剂量反应曲线确定。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-ERK / p-SAPK / p-JNK PARP / cleaved-PARP / pro-caspase3 / cleaved-caspase3 / Bcl-2 Cyclin D / CDK6 / CDK4 / SKP2 LC3A / LC3B |
|
29285232 | |
| Growth inhibition assay | Cell number Cell viability |
|
29069775 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | SCH66336 抑制HTBI77人肺癌裸鼠移植模型中的瘤生长，抑制作用呈剂量依赖性[1]。在NOD/SCID免疫缺陷小鼠皮下注射XEN01, XEN05或XEN08 GBM建立肿瘤移植模型，SCH66336 以 50 mg/kg剂量口服灌胃21天后，可抑制肿瘤生长，抑制率高达69%[3]。 | |
|---|---|---|
| 动物实验 | Animal Models | 6–12周龄NOD/SCID 小鼠 |
| Dosages | 50 mg/kg | |
| Administration | 口服 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05953545 | Not yet recruiting | Chronic Hepatitis Delta |
National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC) |
May 15 2024 | Phase 2 |
| NCT02579044 | Enrolling by invitation | Progeria |
Boston Children''s Hospital |
December 2015 | Phase 1|Phase 2 |
| NCT02430181 | Completed | Chronic Hepatitis D Infection |
Eiger BioPharmaceuticals |
November 2014 | Phase 2 |
| NCT01495585 | Completed | Hepatitis D |
National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC) |
December 2011 | Phase 2 |
| NCT01232881 | Terminated | Breast Cancer |
Hoosier Cancer Research Network|United States Department of Defense|Indiana University School of Medicine|Emory University |
August 2009 | -- |
| NCT00916747 | Active not recruiting | Progeria |
Boston Children''s Hospital|Schering-Plough|Merck Sharp & Dohme LLC|Eiger BioPharmaceuticals |
August 2009 | Phase 2 |
化学信息&溶解度
| 分子量 | 638.82 | 分子式 | C27H31Br2ClN4O2 |
| CAS号 | 193275-84-2 | SDF | Download Lonafarnib (SCH66336) SDF |
| Smiles | C1CN(CCC1CC(=O)N2CCC(CC2)C3C4=C(CCC5=C3N=CC(=C5)Br)C=C(C=C4Br)Cl)C(=O)N | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 127 mg/mL ( (198.8 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 127 mg/mL (198.8 mM) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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