Lonafarnib

For research use only. Not for use in humans.

目录号:S2797 别名: SCH66336

Lonafarnib Chemical Structure

CAS No. 193275-84-2

Lonafarnib (SCH66336) 是一种口服生物有效的FPTase抑制剂,作用于H-rasK-ras-4BN-ras,无细胞试验中IC50分别为1.9 nM, 5.2 nM和2.8 nM。Phase 3。

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10mM (1mL in DMSO) RMB 3509.73 现货
RMB 1416.91 现货
RMB 2229.57 现货
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客户使用Selleck生产的Lonafarnib发表文献11篇:

客户使用该产品的2个实验数据:

  • Huh-7/hNTCP cells were infected with in vitro generated HDV in the presence or absence of MyrB (50 nM) or lonafarnib (200 nM). After 5 days cells were labeled with HDAg#280, secondary AF488 and stained with DAPI. A representative of four independent experiments is shown.

    Antiviral Res, 2017, 141:116-123. Lonafarnib purchased from Selleck.

    Low-dose lonafarnib decreased HIF-1α expression without inhibiting cell growth in MDA-MB-231 cells. (A, B) Lonafarnib (1 μM) treatment for 24 h significantly decreased HIF-1α expression, which was normalized to that of GAPDH. In contrast, lonafarnib (1 μM) did not decrease HIF-2α expression.

    J Cell Physiol, 2017, 232(1):192-201. Lonafarnib purchased from Selleck.

产品安全说明书

Transferase抑制剂选择性比较

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-rasK-ras-4BN-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
H-ras [1]
(Cell-free assay)
N-ras [1]
(Cell-free assay)
K-ras-4B [1]
(Cell-free assay)
1.9 nM 2.8 nM 5.2 nM
体外研究

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Cos-1 monkey kidney cells NWXGZ4s5TnWwY4Tpc44h[XO|YYm= MWfJcohq[mm2aX;uJI9nKFC{b4TlbY4h\mG{bnXzfYx1emGwc3\ldoF{\SCrbjDDc5MuOSCvb37r[Zkhc2mmbnX5JINmdGy|IHX4dJJme3OrbnegTE1T[XNvdnHsMEBKSzVyPUCuNFAyQSEQvF2= NGOwe4wyOjF7MEOwPS=>
COS-7 monkey cells M1TDbWZ2dmO2aX;uJIF{e2G7 M4Xn[WlvcGmkaYTpcochfGinIH\hdo5me3muYYTpc44hd2ZiSD3yZZMheHKxdHXpcpMhcW5iQ1;TMVchdW:wa3X5JINmdGy|IITyZY5{cWWwdHz5JIV5eHKnc4PpcochUC2{YYPbWoFtOTKfLVPWUHMhcW5idHjlJJdpd2ynIHPlcIwh[XO|YYmsJGlEPTB;MD6wNUDPxE1? NXra[nFIQTh{MkW1PC=>
MCF-7 tumor cell line NV\WVG0yT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml3hR49ueG:3bnSge4F{KG2nYYP1doVlKG[xcjDpcohq[mm2aX;uJI9nKE2FRj23JJR2dW:{IHPlcIwhdGmwZTDpckBjemWjc4SgeY5l\XJic3;meEBi\2G{IHHzd4F6NCCLQ{WwQVAvODVizszN MX[5PFIzPTV6
HCT116 M1ezRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXzldI1ZS2:vcH;1coQhf2G|IH3lZZN2emWmIH\vdkBqdmirYnn0bY9vKG:oIFjDWFEyPiC2dX3vdkBk\WyuIHzpcoUhcW5iY3;sc44hfW6mZYKgd49nfCCjZ3HyJIF{e2G7LDDJR|UxRTBwMEeg{txO MnHuPVgzOjV3OB?=
NIH-H tumor cell lines NEi1XHpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmTuR49ueG:3bnSgZYJqdGm2eTD0c{BqdmirYnn0JIFv[2ixcnHn[U1qdmSncHXu[IVvfCCpcn;3eIghd2ZiTlnIMWghfHWvb4KgZ4VtdCCuaX7ld{BqdiC|b3\0JIFo[XJuIFnDOVA:OC5yN{Kg{txO M4rTTVk5OjJ3NUi=
NIH3T3 cells NXPGXJFOTnWwY4Tpc44h[XO|YYm= MYLJcohq[mm2aX;uJI9nKFKjczDmZZJv\XO7bHH0bY9vKGmwIFitVoF{KHS{YX7z[o9zdWWmIF7JTFNVOyClZXzsd{whTUN3ME2wMlEh|ryP NV;SVYlWOTV2NUSyNlg>
NIH-K tumor cell lines MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYDDc41xd3WwZDDhZoltcXS7IITvJIlvcGmkaYSgZY5kcG:{YXflMYlv\GWyZX7k[Y51KGe{b4f0bEBw\iCQSVitT{B1fW2xcjDj[YxtKGyrbnXzJIlvKHOxZoSgZYdieixiSVO1NF0xNjVizszN MWe5PFIzPTV6

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-ERK / p-SAPK / p-JNK; 

PubMed: 29285232     


Western blot analysis of protein levels of phosphoERK1/2, phospho-SAPK/JNK, total ERK1/2 and total SAPK/JNK in HCC cells treated with lonafarnib as indicated.

PARP / cleaved-PARP / pro-caspase3 / cleaved-caspase3 / Bcl-2; 

PubMed: 29285232     


Western blot analysis of levels of apoptosis-related protein including PARP, cleaved PARP, pro-Caspase-3, cleaved Caspase-3 and Bcl-2 in HCC cells treated with lonafarnib as indicated. The asterisk indicates a non-specific band.

Cyclin D / CDK6 / CDK4 / SKP2; 

PubMed: 29285232     


Western blot analysis of levels of cell cycle-related proteins including Cyclin D, CDK4, CDK6 and SKP2 in HCC cells treated with lonafarnib as indicated.

LC3A / LC3B ; 

PubMed: 29069775     


Lonafarnib, inhibitor for farnesyl transferase, significantly induced the expression of autophagy marker.

29285232 29069775
Growth inhibition assay
Cell number; 

PubMed: 29069775     


Lonafarnib, inhibitor for farnesyl transferase, significantly inhibited the cell proliferation. 

Cell viability; 

PubMed: 15860663     


PLC1 cells were treated with the indicated concentrations of SCH66336 for the indicated amount of time. Viability is expressed as the percentage of trypan blue-excluding cells of the total number of cells present. 

29069775 15860663
体内研究 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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[2]
- 合并
  • Cell lines: UMSCC10B, UMSCC14B, UMSCC17B, UMSCC22B, 和UMSCC35, UMSCC38 细胞
  • Concentrations: 0.1 μM - 8 μM
  • Incubation Time: 24 小时
  • Method: 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。
    (Only for Reference)
动物实验:[3]
- 合并
  • Animal Models: 6–12周龄NOD/SCID 小鼠
  • Dosages: 50 mg/kg
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 127 mg/mL (198.8 mM)
Ethanol 127 mg/mL (198.8 mM)
Water Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 638.82
化学式

C27H31Br2ClN4O2

CAS号 193275-84-2
储存条件 粉状
溶于溶剂
别名 SCH66336

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02579044 Enrolling by invitation Drug: Everolimus and lonafarnib Progeria Boston Children''s Hospital December 2015 Phase 1|Phase 2
NCT02527707 Completed Drug: lonafarnib|Drug: Ritonavir Chronic Delta Hepatitis Eiger BioPharmaceuticals|Hannover Medical School September 2015 Phase 2
NCT02430194 Completed Drug: lonafarnib|Drug: Ritonavir|Drug: PEG IFN-a Chronic Hepatitis D Infection Eiger BioPharmaceuticals|Ankara University December 2014 Phase 2
NCT02430181 Completed Drug: lonafarnib|Drug: PEG IFN-a|Drug: Ritonavir Chronic Hepatitis D Infection Eiger BioPharmaceuticals November 2014 Phase 2
NCT01495585 Completed Drug: Lonafarnib|Other: Placebo 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 Procedure: Tumor Sample|Procedure: Serum Sample Breast Cancer Hoosier Cancer Research Network|United States Department of Defense|Indiana University School of Medicine|Emory University August 2009 --

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Transferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID