Lonafarnib

Name: Lonafarnib
Brand: Tocris Bioscience
SKU: 6265

Tocris Bioscience, part of Bio-Techne | Catalog # 6265

Citations (4)

COA / SDS

Potent farnesyltransferase inhibitor

Key Product Details

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)
Molecular Weight:	638.82

View Full Technical Details for Lonafarnib

Technical Data
Citations

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 for Lonafarnib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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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References for Lonafarnib

References are publications that support the biological activity of the 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