2. Metabolic Enzyme/Protease GPCR/G Protein Autophagy
  3. Farnesyl Transferase Ras Autophagy
  4. Lonafarnib

Lonafarnib  (Synonyms: Sch66336)

Cat. No.: HY-15136 Purity: 98.67%
COA Handling Instructions

Lonafarnib (Sch66336) is a potent and orally active farnesyl transferase (FTase) inhibitor. Lonafarnib inhibits the activities of H-ras, K-ras and N-ras with IC50 values of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib also has anti-hepatitis delta virus (HDV) activities.

For research use only. We do not sell to patients.

Lonafarnib Chemical Structure

Lonafarnib Chemical Structure

CAS No. : 193275-84-2

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 205 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 205 In-stock
Solid
5 mg USD 120 In-stock
10 mg USD 190 In-stock
25 mg USD 380 In-stock
50 mg USD 600 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Lonafarnib:

Lonafarnib Related Antibodies

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K-Ras H-Ras Ras

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Lonafarnib (Sch66336) is a potent and orally active farnesyl transferase (FTase) inhibitor. Lonafarnib inhibits the activities of H-ras, K-ras and N-ras with IC50 values of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib also has anti-hepatitis delta virus (HDV) activities.

IC50 & Target

IC50: 1.9 nM (H-ras), 5.2 nM (K-ras), 2.8 nM (N-ras)[1]
In Vitro

Lonafarnib (Sch66336) potently inhibits Ha-Ras processing in whole cells and blocks the trans formed growth properties of fibroblasts and human tumor cell lines expressing activated Ki-Ras proteins[1]. All treatment groups containing Lonafarnib (10 μM) show a significantly higher level of unfarnesylated H-Ras (116-137%) compared to control treatment[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Lonafarnib Related Antibodies
In Vivo

In mouse, rat, and monkey systems, Lonafarnib (Sch66336) has excellent oral bioavailability and pharmacokinetic properties. In the nude mouse, Lonafarnib demonstrates potent oral activity in a wide array of human tumor xenograft models including tumors of colon, lung, pancreas, prostate, and urinary bladder origin[1]. Lonafarnib alone (80 mg/kg by oral gavage, once daily) has limited ability to inhibit orthotopic U87 tumors compared to vehicle treated control animals (T/C of 0.67). The combination of XRT/Tem (2.5Gy/day for 2 days; 5 mg/kg by oral gavage 90 min prior to XRT) is designed to produce modest tumor growth inhibition in vivo(T/C of 0.42). Concurrent Lonafarnib/XRT/Tem (Lonafarnib 80 mg/kg by oral gavage, once daily, XRT 2.5Gy/day for 2 days, and Tem 5 mg/kg by oral gavage 90 min prior to XRT) provides the strongest growth reduction (T/C of 0.02) and is significantly more effective than XRT/Tem (p<0.04), with the majority of animals demonstrating a decrease in tumor volume (p<0.05) after two weeks and persisting after 4 weeks (p<0.05)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

638.82

Appearance

Solid

Formula

C27H31Br2ClN4O2
CAS No.
SMILES

O=C(N1CCC(CC(N2CCC([C@@H]3C4=C(Br)C=C(Cl)C=C4CCC5=CC(Br)=CN=C53)CC2)=O)CC1)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (78.27 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5654 mL 7.8269 mL 15.6539 mL
5 mM 0.3131 mL 1.5654 mL 3.1308 mL
10 mM 0.1565 mL 0.7827 mL 1.5654 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.91 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.91 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.91 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 98.67%

COA (254 KB) LCMS (116 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

FPTactivity is determined by measuring the transfer of [3H]farnesyl from [3H]farnesyl PPi to trichloroacetic acid-precipitable Ha-Ras-CVLS. GGPT-1 activity is similarly determined using [3H]geranylgeranyl diphosphate and Ha-Ras-CVLL as substrates[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

CellTiter96 Aqueous Assay kit is used. Assays are performed with 5000 cells/well in a 96-well tissue culture plate. Plates are irradiated 24 h after drug exposure and assayed 96 h after XRT, with fresh drug treatments applied each day. For quantification, dye is added directly to each well, plates are washed as per the manufactures recommendation and cell viability determined by optical density. Significance is analyzed using the Student’s T-test. 12-well plates are seeded with 100,000 cells/well. Drug treatments are initiated 24 h after plating, and media is replaced every 24 h for a total of 96 h of drug exposure. Plates are irradiated after 24 h of drug exposure. Cells from triplicate sets of treatments are trypsonized and counted 48 h after irradation using a Z1 series coulter counter, and compared to cell numbers from wells counted on Day 1 (the day drug treatment is initiated). Proliferation after drug treatments are normalized to the control wells and expressed as % of the control treatment. Significance is analyzed using the Student’s T-test[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice[2]
Lonafarnib is given once daily at 80mg/kg with twice weekly weightings to ensure accurate dosing. Temozolomide (Tem) is given by gavage at 5 mg/kg 90 min prior to XRT. For irradiation, anesthetized mice are placed in a lead shielding apparatus which limited radiation exposure to the head only. Treatment (2.5Gy/day for two days) is delivered using a Gammacell 40 irradiator delivering 100 rads/min. For in vivo combination experiments, suboptimal doses of XRT/Tem are selected to permit identification of synergistic effects of Lonafarnib.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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Lonafarnib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Lonafarnib193275-84-2Sch66336Sch 66336Sch-66336Farnesyl TransferaseRasAutophagyFtaseInhibitorinhibitorinhibit

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