Lonafarnib

Key Product Details

Product Description

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.

Product Specifications for Lonafarnib

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

2 1 Recalculate

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

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 3 publications citing the usage of this product.

• Shen Farnesyltransferase and geranylgeranyltransferase I: structures, mechanism, inhibitors and molecular modeling. Drug Discov.Today. 2015 PMID: 25450772
• Nielsen Combination therapy with the farnesyl protein transferase inhibitor SCH66336 and SCH58500 (p53 adenovirus) in preclinical cancer models. Cancer Res. 1999 PMID: 10606231
• Wang The farnesyl protein transferase inhibitor SCH66336 is a potent inhibitor of MDR1 product P-glycoprotein. Cancer.Res. 2001 PMID: 11606389
• Sun Lonafarnib is a potential inhibitor for neovascularization. PLoS One. 2015 PMID: 25853815
• Lo Cicero A high throughput phenotypic screening reveals compounds that counteract premature osteogenic differentiation of HGPS iPS-derived mesenchymal stem cells. Sci.Rep. 2016 PMID: 27739443
• Bowman Phosphorylation of FADD by the kinase CK1α promotes KRASG12D-induced lung cancer. Sci.Signal. 2015 PMID: 25628462

Product Documents for Lonafarnib