Lonafarnib

For research use only.

Catalog No.S2797 Synonyms: SCH66336

13 publications

Lonafarnib Chemical Structure

CAS No. 193275-84-2

Lonafarnib (SCH66336) 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.

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Selleck's Lonafarnib has been cited by 13 publications

2 Customer Reviews

  • 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.

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Biological Activity

Description Lonafarnib (SCH66336) 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.
Targets
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
In vitro

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Cos-1 monkey kidney cells NULWWHU3TnWwY4Tpc44h[XO|YYm= M3j5O2lvcGmkaYTpc44hd2ZiUILveIVqdiCoYYLu[ZN6dHS{YX7z[oVz[XOnIHnuJGNwey1zIH3vcotmgSCtaXTu[Zkh[2WubIOg[ZhxemW|c3nu[{BJNVKjcz32ZYwtKEmFNUC9NE4xODF7IN88US=> NEG1NY8yOjF7MEOwPS=>
COS-7 monkey cells MYLGeY5kfGmxbjDhd5NigQ>? MnG4TY5pcWKrdHnu[{B1cGViZnHycoV{gWyjdHnvckBw\iCKLYLhd{Bxem:2ZXnud{BqdiCFT2OtO{Bud26tZYmgZ4VtdHNidILhcpNq\W62bImg[ZhxemW|c3nu[{BJNXKjc2vWZYwyOl1vQ2\MV{BqdiC2aHWge4hwdGViY3XscEBie3OjeTygTWM2OD1yLkCxJO69VQ>? NUT6ZlJjQTh{MkW1PC=>
MCF-7 tumor cell line NFn1Z3FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUPDc41xd3WwZDD3ZZMhdWWjc4Xy[YQh\m:{IHnubIljcXSrb36gc4YhVUOILUegeJVud3JiY3XscEBtcW6nIHnuJIJz\WG|dDD1coRmeiC|b3\0JIFo[XJiYYPzZZktKEmFNUC9NE4xPSEQvF2= MWK5PFIzPTV6
HCT116 NFTjNo1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1LDS2NwdXCxdX7kJJdieyCvZXHzeZJm\CCob4KgbY5pcWKrdHnvckBw\iCKQ2SxNVYhfHWvb4KgZ4VtdCCuaX7lJIlvKGOxbH;uJJVv\GW{IIPv[pQh[WejcjDhd5NigSxiSVO1NF0xNjB5IN88US=> MonIPVgzOjV3OB?=
NIH-H tumor cell lines NFn3eZVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkT0R49ueG:3bnSgZYJqdGm2eTD0c{BqdmirYnn0JIFv[2ixcnHn[U1qdmSncHXu[IVvfCCpcn;3eIghd2ZiTlnIMWghfHWvb4KgZ4VtdCCuaX7ld{BqdiC|b3\0JIFo[XJuIFnDOVA:OC5yN{Kg{txO MljLPVgzOjV3OB?=
NIH3T3 cells MX\GeY5kfGmxbjDhd5NigQ>? NUf1SHY5UW6qaXLpeIlwdiCxZjDSZZMh\mG{bnXzfYxifGmxbjDpckBJNVKjczD0doFve2[xcn3l[EBPUUh|VEOgZ4VtdHNuIFXDOVA:OC5zIN88US=> NFrTcnoyPTR3NEKyPC=>
NIH-K tumor cell lines NIO3O45Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkizR49ueG:3bnSgZYJqdGm2eTD0c{BqdmirYnn0JIFv[2ixcnHn[U1qdmSncHXu[IVvfCCpcn;3eIghd2ZiTlnIMWshfHWvb4KgZ4VtdCCuaX7ld{BqdiC|b3\0JIFo[XJuIFnDOVA:OC53IN88US=> MofnPVgzOjV3OB?=

... 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
In vivo 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]

Protocol

Cell Research:[2]
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  • Cell lines: UMSCC10B, UMSCC14B, UMSCC17B, UMSCC22B, and UMSCC35, UMSCC38 cell lines
  • Concentrations: 0.1 μM - 8 μM
  • Incubation Time: 24 hours
  • Method: 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.
    (Only for Reference)
Animal Research:[3]
- Collapse
  • Animal Models: NOD/SCID mice between 6–12 weeks of age
  • Dosages: 50 mg/kg
  • Administration: p.o. bid by oral gavage
    (Only for Reference)

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 638.82
Formula

C27H31Br2ClN4O2
CAS No. 193275-84-2
Storage powder
in solvent
Synonyms SCH66336
Smiles C1CN(CCC1CC(=O)N2CCC(CC2)C3C4=C(CCC5=C3N=CC(=C5)Br)C=C(C=C4Br)Cl)C(=O)N

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Clinical Trial Information

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID