Lonafarnib

Catalog No.S2797 Synonyms: SCH66336

Lonafarnib Chemical Structure

Molecular Weight(MW): 638.82

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.

Size Price Stock Quantity  
In DMSO USD 430 In stock
USD 170 In stock
USD 270 In stock
Bulk Discount
Bulk Inquiry

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 5 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.

Purity & Quality Control

Choose Selective Transferase Inhibitors

Biological Activity

Description 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.
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 MXXGeY5kfGmxbjDhd5NigQ>? NYHqdoJyUW6qaXLpeIlwdiCxZjDQdo91\WmwIH\hdo5me3mudILhcpNn\XKjc3WgbY4hS2:|LUGgcY9vc2W7IHvp[I5mgSClZXzsd{BmgHC{ZYPzbY5oKEhvUnHzMZZidCxiSVO1NF0xNjByMUmg{txO MXqxNlE6ODNyOR?=
COS-7 monkey cells M{\WZmZ2dmO2aX;uJIF{e2G7 NX;UR4hzUW6qaXLpeIlv\yC2aHWg[oFzdmW|eXzheIlwdiCxZjDIMZJieyCycn;0[YlveyCrbjDDU3MuPyCvb37r[Zkh[2WubIOgeJJidnOrZX70cJkh\XiycnXzd4lv\yCKLYLhd3tX[WxzMm2tR3ZNWyCrbjD0bIUhf2ixbHWgZ4VtdCCjc4PhfUwhUUN3ME2wMlAyKM7:TR?= MYG5PFIzPTV6
MCF-7 tumor cell line MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFrzSXVEd22yb4Xu[EB4[XNibXXhd5Vz\WRiZn;yJIlvcGmkaYTpc44hd2ZiTVPGMVchfHWvb4KgZ4VtdCCuaX7lJIlvKGK{ZXHzeEB2dmSncjDzc4Z1KGGpYYKgZZN{[XluIFnDOVA:OC5yNTFOwG0> NUjDTVZ2QTh{MkW1PC=>
HCT116 MkXKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVfYWFlES2:vcH;1coQhf2G|IH3lZZN2emWmIH\vdkBqdmirYnn0bY9vKG:oIFjDWFEyPiC2dX3vdkBk\WyuIHzpcoUhcW5iY3;sc44hfW6mZYKgd49nfCCjZ3HyJIF{e2G7LDDJR|UxRTBwMEeg{txO MVu5PFIzPTV6
NIH-H tumor cell lines MmX3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVLDc41xd3WwZDDhZoltcXS7IITvJIlvcGmkaYSgZY5kcG:{YXflMYlv\GWyZX7k[Y51KGe{b4f0bEBw\iCQSVitTEB1fW2xcjDj[YxtKGyrbnXzJIlvKHOxZoSgZYdieixiSVO1NF0xNjB5MjFOwG0> M2nZ[Vk5OjJ3NUi=
NIH3T3 cells M13mZ2Z2dmO2aX;uJIF{e2G7 NHWzWlZKdmirYnn0bY9vKG:oIGLhd{Bn[XKwZYP5cIF1cW:wIHnuJGguWmG|IITyZY5{\m:{bXXkJG5KUDOWMzDj[YxteyxiRVO1NF0xNjFizszN M2m2RlE2PDV2MkK4
NIH-K tumor cell lines NH7sbVhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1uxe2NwdXCxdX7kJIFjcWyrdImgeI8hcW6qaXLpeEBidmOqb4Lh[4UucW6mZYDlcoRmdnRiZ4Lve5RpKG:oIF7JTE1MKHS3bX;yJINmdGxibHnu[ZMhcW5ic3;meEBi\2G{LDDJR|UxRTBwNTFOwG0> MkG3PVgzOjV3OB?=

... Click to View More Cell Line Experimental Data
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]
+ Expand
  • 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]
+ Expand
  • Animal Models: NOD/SCID mice between 6–12 weeks of age
  • Formulation: 20% (w/v) HPβCD
  • 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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02511431 Completed Hepatitis D National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC) July 29 2015 Phase 2
NCT02968641 Not yet recruiting Chronic Delta Hepatitis Eiger BioPharmaceuticals March 2017 Phase 2
NCT02579044 Recruiting Progeria Boston Children’s Hospital December 2015 Phase 1|Phase 2
NCT02527707 Completed Chronic Delta Hepatitis Eiger BioPharmaceuticals|Hannover Medical School September 2015 Phase 2
NCT02430194 Completed Chronic Hepatitis D Infection Eiger BioPharmaceuticals|Ankara University December 2014 Phase 2
NCT02430181 Completed Chronic Hepatitis D Infection Eiger BioPharmaceuticals November 2014 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field
selleck catalog

Transferase Signaling Pathway Map
Tags: buy Lonafarnib | Lonafarnib supplier | purchase Lonafarnib | Lonafarnib cost | Lonafarnib manufacturer | order Lonafarnib | Lonafarnib distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID