Lonafarnib|Ftase inhibitor,potent and selective|CAS# 193275-84-2

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Size	Price	Stock
10mM (in 1mL DMSO)	$170.00	In stock
5mg	$119.00	In stock
10mg	$189.00	In stock
100mg	$1,309.00	In stock
200mg	$1,939.00	In stock

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Quality Control

Quality Control & MSDS

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Purity = 99.65%

Chemical structure

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)

Protocol

Cell experiment [1]:
Cell lines	UMSCC10B, UMSCC14B, UMSCC17B, UMSCC22B, UMSCC35 and UMSCC38 cells
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
Applications	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
Applications	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.
References: [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.

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Chemical Properties

Cas No.	193275-84-2	SDF	Download SDF
Synonyms	Sch 66336, Sch66336, Sch-66336
Chemical Name	4-[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
Canonical SMILES	C1CN(CCC1CC(=O)N2CCC(CC2)C3C4=C(C=C(C=C4CCC5=CC(=CN=C35)Br)Cl)Br)C(=O)N
Formula	C₂₇H₃₁Br₂ClN₄O₂	M.Wt	638.82
Solubility	>32mg/mL in DMSO	Storage	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

Background

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]

Reference

[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.