For research use only. Not for use in humans.

製品コードS2797 別名:SCH66336



Lonafarnib is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Phase 3.

サイズ 価格(税別) 在庫  
10mM (1mL in DMSO) JPY 73300 あり
JPY 30200 あり
JPY 46800 あり

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  • 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.




製品説明 Lonafarnib is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Phase 3.
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

SCH66336 at concentration ranging from 0.1 μM to 8 μM suppress growth and induce apoptosis of human head and neck squamous carcinoma cells (HNSCC) in a dose and time dependent manner. SCH66336 (8 μM) suppresses protein kinase B/Akt activity as well as the phosphorylation of the Akt substrates glycogen synthase kinase (GSK)-3β, forkhead transcription factor, and BAD in SqCC/Y1 cells. [2] SCH66336 demonstrate variable antiproliferative effects against the cell lines, with IC50 ranging from 0.6 μM to 32.3 μM. [3] Lonafarnib induces a CCAAT/enhancer-binding protein homologous protein (CHOP)-dependent transactivation of the DR5 promoter, thus induces CHOP-dependent DR5 up-regulation. Lonafarnib (< 10 μM) activates caspase-8 and its downstream caspases, thus induces caspase-8-dependent apoptosis in H1792 cells. Lonafarnib (5 μM) up-regulate DR5 expression, increase cell-surface DR5 distribution, and enhance tumor necrosis factor-related apoptosis-inducing ligand-induced apoptosis in H1792 cells.[4]

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Cos-1 monkey kidney cells MWHGeY5kfGmxbjDhd5NigQ>? NWXGW495UW6qaXLpeIlwdiCxZjDQdo91\WmwIH\hdo5me3mudILhcpNn\XKjc3WgbY4hS2:|LUGgcY9vc2W7IHvp[I5mgSClZXzsd{BmgHC{ZYPzbY5oKEhvUnHzMZZidCxiSVO1NF0xNjByMUmg{txO M{PyVVEzOTlyM{C5
COS-7 monkey cells NUL3ToRlTnWwY4Tpc44h[XO|YYm= MYnJcohq[mm2aX7nJJRp\SCoYYLu[ZN6dGG2aX;uJI9nKEhvcnHzJJBzd3SnaX7zJIlvKEORUz23JI1wdmuneTDj[YxteyC2cnHud4lmdnSueTDlfJBz\XO|aX7nJGguemG|W2\hcFEzZS2FVlzTJIlvKHSqZTD3bI9t\SClZXzsJIF{e2G7LDDJR|UxRTBwMEGg{txO NGrTelI6QDJ{NUW4
MCF-7 tumor cell line MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3;Zc2NwdXCxdX7kJJdieyCvZXHzeZJm\CCob4KgbY5pcWKrdHnvckBw\iCPQ1[tO{B1fW2xcjDj[YxtKGyrbnWgbY4h[nKnYYP0JJVv\GW{IIPv[pQh[WejcjDhd5NigSxiSVO1NF0xNjB3IN88US=> NEPVVZQ6QDJ{NUW4
HCT116 NUDSZWhST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWnDc41xd3WwZDD3ZZMhdWWjc4Xy[YQh\m:{IHnubIljcXSrb36gc4YhUEOWMUG2JJR2dW:{IHPlcIwhdGmwZTDpckBkd2yxbjD1coRmeiC|b3\0JIFo[XJiYYPzZZktKEmFNUC9NE4xPyEQvF2= MmqyPVgzOjV3OB?=
NIH-H tumor cell lines Mo\VS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2HEPWNwdXCxdX7kJIFjcWyrdImgeI8hcW6qaXLpeEBidmOqb4Lh[4UucW6mZYDlcoRmdnRiZ4Lve5RpKG:oIF7JTE1JKHS3bX;yJINmdGxibHnu[ZMhcW5ic3;meEBi\2G{LDDJR|UxRTBwMEeyJO69VQ>? MojMPVgzOjV3OB?=
NIH3T3 cells M{TzfGZ2dmO2aX;uJIF{e2G7 MVTJcohq[mm2aX;uJI9nKFKjczDmZZJv\XO7bHH0bY9vKGmwIFitVoF{KHS{YX7z[o9zdWWmIF7JTFNVOyClZXzsd{whTUN3ME2wMlEh|ryP M1\IUFE2PDV2MkK4
NIH-K tumor cell lines M{nKbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXvDc41xd3WwZDDhZoltcXS7IITvJIlvcGmkaYSgZY5kcG:{YXflMYlv\GWyZX7k[Y51KGe{b4f0bEBw\iCQSVitT{B1fW2xcjDj[YxtKGyrbnXzJIlvKHOxZoSgZYdieixiSVO1NF0xNjVizszN NG[0U4Y6QDJ{NUW4


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
体内試験 SCH66336 inhibits HTBI77 human lung carcinoma xenograft growth in nude mice in a dose-dependent fashion. [1] SCH66336 dosed at 50 mg/kg p.o. bid by oral gavage inhibits tumor growth with up to 69% growth inhibition after 21 days of treatment in NOD/SCID mice bearing s.c. flank XEN01, XEN05 or XEN08 GBM xenografts. [3]


細胞試験: [2]
- 合併
  • 細胞株: UMSCC10B, UMSCC14B, UMSCC17B, UMSCC22B, and UMSCC35, UMSCC38 cell lines
  • 濃度: 0.1 μM - 8 μM
  • 反応時間: 24 hours
  • 実験の流れ: The cells are seeded in 96-well cell-culture cluster plates at a density that allowed control cultures to grow exponentially for 5 days. After 24 hours, the cells are treated with different concentrations of SCH66336. SCH66336 is dissolved in DMSO. Control cultures received the same amount of DMSO as the treated cultures do. Cell numbers are estimated after 5 days of treatment by SRB assay. The percentage of growth inhibition is calculated by using the equation: percentage growth inhibition = (1 − At/Ac) × 100, where At and Ac represent the absorbance in treated and control cultures, respectively. The drug concentration causing a 50% cell growth inhibition (IC50), is determined by interpolation from dose-response curves.
- 合併
  • 動物モデル: NOD/SCID mice between 6–12 weeks of age
  • 投薬量: 50 mg/kg
  • 投与方法: p.o. bid by oral gavage

溶解度 (25°C)

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

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。


分子量 638.82


CAS No. 193275-84-2
in solvent
別名 SCH66336
Smiles NC(=O)N1CCC(CC1)CC(=O)N2CCC(CC2)C3C4=C(CCC5=C3C(=CC(=C5)Cl)Br)C=C(Br)C=N4


投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
% DMSO % % Tween 80 % ddH2O





質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)


  • 質量





開始濃度 x 開始体積 = 最終濃度 x 最終体積


この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1



  • 連続希釈剤

  • 計算結果

  • 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):




チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2


質量 濃度 体積 分子量


NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02579044 Recruiting 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 --



Handling Instructions


  • * 必須


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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID