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Submit ReviewLonafarnib
Description: Potent farnesyltransferase inhibitor
Chemical Name: 4-[2-[4-[(11R)-3,10-Dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl]-1-piperidinyl]-2-oxoethyl]-1-piperidinecarboxamide
Purity: ≥98% (HPLC)
Biological Activity for Lonafarnib
Lonafarnib is a potent farnesyl transferase inhibitor (IC50 = 1.9 nM). Inhibits farnesylation of RAS. Also inhibits Pgp transport (IC50 < 3 μM) and increases potency and anticancer activity when used in conjunction with cytotoxic Pgp substrates. Inhibits neovascularization by affecting cell motility. Orally bioavailable.
Technical Data for Lonafarnib
| M. Wt | 638.82 |
| Formula | C27H31Br2ClN4O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 193275-84-2 |
| PubChem ID | 148195 |
| InChI Key | DHMTURDWPRKSOA-RUZDIDTESA-N |
| Smiles | NC(N1CCC(CC1)CC(N2CCC([C@H]3C4=NC=C(C=C4CCC5=CC(Cl)=CC(Br)=C35)Br)CC2)=O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Lonafarnib
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 6.39 | 10 |
Preparing Stock Solutions for Lonafarnib
The following data is based on the product molecular weight 638.82. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 15.65 mL | 78.27 mL | 156.54 mL |
| 0.5 mM | 3.13 mL | 15.65 mL | 31.31 mL |
| 1 mM | 1.57 mL | 7.83 mL | 15.65 mL |
| 5 mM | 0.31 mL | 1.57 mL | 3.13 mL |
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Product Datasheets for Lonafarnib
References for Lonafarnib
References are publications that support the biological activity of the product.
Bowman et al (2015) Phosphorylation of FADD by the kinase CK1α promotes KRASG12D-induced lung cancer. Sci.Signal. 8 PMID: 25628462
Lo Cicero et al (2016) A high throughput phenotypic screening reveals compounds that counteract premature osteogenic differentiation of HGPS iPS-derived mesenchymal stem cells. Sci.Rep. 6 34798 PMID: 27739443
Sun et al (2015) Lonafarnib is a potential inhibitor for neovascularization. PLoS One. 10 e0122830 PMID: 25853815
Wang et al (2001) The farnesyl protein transferase inhibitor SCH66336 is a potent inhibitor of MDR1 product P-glycoprotein. Cancer.Res. 61 7525 PMID: 11606389
Nielsen et al (1999) Combination therapy with the farnesyl protein transferase inhibitor SCH66336 and SCH58500 (p53 adenovirus) in preclinical cancer models. Cancer Res. 59 5896 PMID: 10606231
Shen et al (2015) Farnesyltransferase and geranylgeranyltransferase I: structures, mechanism, inhibitors and molecular modeling. Drug Discov.Today. 20 267 PMID: 25450772
If you know of a relevant reference for Lonafarnib, please let us know.
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Keywords: Lonafarnib, Lonafarnib supplier, Lonafarnib, SCH66336, farnesyl, transferase, inhibitors, inhibits, PgP, transport, anticancer, neovascularization, orally, bioavailable, Protein, Prenyltransferases, Post-translational, Modifications, 6265, Tocris Bioscience
1 Citation for Lonafarnib
Citations are publications that use Tocris products. Selected citations for Lonafarnib include:
Daniel E et al (2022) Progerin-expressing endothelial cells are unable to adapt to shear stress. Biophys J 121 620-628 PMID: 34999130
Do you know of a great paper that uses Lonafarnib from Tocris? Please let us know.
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