Lonafarnib

Pricing Availability Delivery Time Qty
Cat.No. 6265 - Lonafarnib | C27H31Br2ClN4O2 | CAS No. 193275-84-2
Description: Potent farnesyl transferase 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)
Datasheet
Citations
Literature

Biological Activity

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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 6.39 10mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 638.82. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.57 mL 7.83 mL 15.65 mL
5 mM 0.31 mL 1.57 mL 3.13 mL
10 mM 0.16 mL 0.78 mL 1.57 mL
50 mM 0.03 mL 0.16 mL 0.31 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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: 5450772


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Keywords: Lonafarnib, supplier, Lonafarnib, SCH66336, farnesyl, transferase, inhibitors, inhibits, PgP, transport, anticancer, neovascularization, orally, bioavailable, Protein, Prenyltransferases, Post-translational, Modifications, Protein, Prenyltransferases, Tocris Bioscience

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Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

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