Lonafarnib
Tocris Bioscience, part of Bio-Techne | Catalog # 6265
Potent farnesyltransferase inhibitor
Key Product Details
Description
Potent farnesyltransferase inhibitor
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
Molecular Weight
638.82
Formula
C27H31Br2ClN4O2
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for Lonafarnib
For research use only
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