Lonafarnib

Lonafarnib (Sch66336) is a potent and orally active farnesyl transferase (FTase) inhibitor. Lonafarnib inhibits the activities of H-ras, K-ras and N-ras with IC50 values of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib also has anti-hepatitis delta virus (HDV) activities.

Product Specifications

CAS Number

[193275-84-2]

Product Name Alternative

Sch66336

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy; Farnesyl Transferase; Ras

Type

Reference compound

Related Pathways

Autophagy; GPCR/G Protein; MAPK/ERK Pathway; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer; Infection

Assay Protocol

https://www.medchemexpress.com/Lonafarnib.html

Purity

99.85

Solubility

DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(N1CCC(CC(N2CCC([C@@H]3C4=C(Br)C=C(Cl)C=C4CCC5=CC(Br)=CN=C53)CC2)=O)CC1)N

Molecular Formula

C27H31Br2ClN4O2

Molecular Weight

638.82

Precautions

H302, H315, H319, H335

References & Citations

[1]Liu M, et al. Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice. Cancer Res. 1998 Nov 1;58 (21) :4947-56.|[2]Chaponis D, et al. Lonafarnib (SCH66336) improves the activity of temozolomide and radiation for orthotopic malignant gliomas. J Neurooncol. 2011 Aug;104 (1) :179-89.|[3]Koh C, et al. Oral prenylation inhibition with lonafarnib in chronic hepatitis D infection: a proof-of-concept randomised, double-blind, placebo-controlled phase 2A trial. Lancet Infect Dis. 2015 Oct;15 (10) :1167-1174.