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Catalog No.
Ftase inhibitor,potent and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
In stock
In stock
In stock
In stock
Ship with 10-15 days

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Lonafarnib (SCH66336, Sarasar) is an potent, selective, orally, bioavailable tricyclic nonpeptidyl nonsulfhydry inhibitor of farnesyltransferase (FTase).[1] It is a small molecular with the formula of C27H31Br2ClN4O2 and molecular weight of 638.82. Farnesylated Ras proteins was found to regulate signal transduction pathways which drive cell proliferation, growth and survival and be required for its membrane localization.[1, 2] Lonafarnib inhibits the post-translational farnesylcation of ras proteins, therefore blocking translocation of RAS to the plasma membrane.[3]


[1] Eric W, Malcolm J. M, Kim N. C, D. Scott E, et al. A multinomial Phase II study of lonafarnib (SCH 66336) in patients with refractory urothelial cancer. Urologic Oncology: Seminars and Original Investigations. 2005, 23. 143-149.

[2] Gongjie L, Stacey A. T, Cindy H. M, Yunsheng H, W. Robert B, et al. Continuous and intermittent dosing of lonafarnib potentiates the therapeutic efficacy of docetaxel on preclinical human prostate cancer models. Int. J. Cancer. 2009, 125. 2711–2720.

[3] Vasiliki A. N, Alexander J. S, Keith T. F, Hensin T, et al. Melanoma: New Insights and New Therapies. J Invest Dermatol. 2012, 132. 854–863.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
Cas No.193275-84-2
SynonymsSch 66336, Sch66336, Sch-66336
Solubility≥31.95 mg/mL in DMSO; insoluble in H2O; ≥96.4 mg/mL in EtOH with ultrasonic
Chemical Name4-[2-[4-[(11R)-3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[1,2]cyclohepta[2,4-b]pyridin-11-yl]piperidin-1-yl]-2-oxoethyl]piperidine-1-carboxamide
SDFDownload SDF
Canonical SMILESC1CN(CCC1CC(=O)N2CCC(CC2)C3C4=C(C=C(C=C4CCC5=CC(=CN=C35)Br)Cl)Br)C(=O)N
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.


Cell experiment [1]:

Cell lines


Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months.

Reaction Conditions

0.1 ~ 8 μM; 24 hrs


In human head and neck squamous carcinoma cells (HNSCCs), SCH66336 (0.1 ~ 8 μM) suppressed cell growth and induced apoptosis of in a dose- and time- dependent manner.

Animal experiment [2]:

Animal models

NOD/SCID mice bearing XEN08 tumors

Dosage form

50 mg/kg; p.o.; b.i.d., for 20 days


In NOD/SCID mice bearing XEN08 tumors, SCH66336 (50 mg/kg, p.o., b.i.d.) significantly inhibited tumor growth, with a mean growth inhibition of 63.8 ± 5.0%.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.


[1]. Chun KH, Lee HY, Hassan K, Khuri F, Hong WK, Lotan R. Implication of protein kinase B/Akt and Bcl-2/Bcl-XL suppression by the farnesyl transferase inhibitor SCH66336 in apoptosis induction in squamous carcinoma cells. Cancer Res. 2003 Aug 15;63(16):4796-800.

[2]. Feldkamp MM, Lau N, Roncari L, Guha A. Isotype-specific Ras.GTP-levels predict the efficacy of farnesyl transferase inhibitors against human astrocytomas regardless of Ras mutational status. Cancer Res. 2001 Jun 1;61(11):4425-31.

Biological Activity

Description Lonafarnib is an inhibitor of farnesyl transferase (FT) with IC50 values of 1.9, 2.8, 5.2 and 10-100 nM for H-Ras, N-Ras, K-Ras and Rheb, respectively.
Targets FT FT FT FT    
IC50 1.9 nM (H-Ras) 2.8 nM (N-Ras) 5.2 nM (K-Ras) 10-100 nM (Rheb)    

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