Lonafarnib

• Description:

  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 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• CAS Number:

  193275-84-2