LONAFARNIB

Product Name: LONAFARNIB
CAS No.: 193275-84-2
Chemical Name: LONAFARNIB
Synonyms: Sarasar;Sch66336;Sch 66336;EOS-61911;LONAFARNIB;LonafarMib;SCH-066336;Unii-iow153004f;Lonafarnib [usan];Valine Impurity 114
CBNumber: CB31011743
Molecular Formula: C27H31Br2ClN4O2
Formula Weight: 638.82
MOL File: 193275-84-2.mol

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LONAFARNIB Property

Melting point:: 214.5-215.9° (monohydrate); mp 222-223°
alpha: D25 = +49.1° (c = 0.21 in methanol)
Boiling point:: 710.4±70.0 °C(Predicted)
Density: 1.536
storage temp.: -20°C
solubility: Chloroform (Slightly), Methanol (Slightly)
pka: 15.76±0.40(Predicted)
form: powder
color: white to beige

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1457
Product name: Lonafarnib
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $131.1
Updated: 2025/07/31

Sigma-Aldrich

Product number: SML1457
Product name: Lonafarnib
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $499
Updated: 2025/07/31

Cayman Chemical

Product number: 11746
Product name: Lonafarnib
Purity: ≥98%
Packaging: 1mg
Price: $33
Updated: 2024/03/01

Cayman Chemical

Product number: 11746
Product name: Lonafarnib
Purity: ≥98%
Packaging: 5mg
Price: $112
Updated: 2024/03/01

Cayman Chemical

Product number: 11746
Product name: Lonafarnib
Purity: ≥98%
Packaging: 10mg
Price: $143
Updated: 2024/03/01

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LONAFARNIB Chemical Properties,Usage,Production

Uses

Chemotherapeutic (farnesyl transfer ase inhibitor).

Uses

Lonafarnib is an orally bioavailable tricyclic inhibitor of farnesyl protein transferase. It inhibits Rheb farnesylation and mTOR signaling and enhances taxane and tamoxifen antitumor activity. Studies show that it induces CCAAT/enhancer-binding protein homologous protein-dependent expression of death receptor 5, leading to induction of apoptosis in human cancer cells

Definition

ChEBI: A 4-{2-[4-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl]-2-oxoethyl}piperidine-1-carboxamide that has R configuration. It is used as oral farnesyltransferase nhibitor.

General Description

Lonafarnib (SCH66336) is a farnesyl transferase inhibitor (FTI). K- and N-Ras are substrates of farnesyl transferase.

Biological Activity

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.

Biochem/physiol Actions

Lonafarnib prevents the post-translational lipid modification of H-Ras and other farnesylated proteins. Lonafarnib treatment results in microtubule bundling, increased microtubule acetylation and stabilization and suppression of microtubule dynamics.

Mechanism of action

Lonafarnib is a protein farnesyltransferase inhibitor (FTI) that reversibly binds to the farnesyltransferase CAAX binding site9, thereby inhibiting progerin farnesylation and subsequent intercalation into the nuclear membrane.

Side effects

vomiting
diarrhea
nausea
stomach pain
constipation
gas
decreased appetite
decreased weight

Synthesis

The two benzylic protons of tricyclic compound 177 were removed in the presence of quinine and mesylate 180 to generate intermediate 181 with excellent conversion and 95% enantiomeric purity (ee). In situ removal of the Boc protecting group under acidic conditions allowed 181 to crystallize as N-acetyl-L-phenylalaninate 182, which was isolated from 177 in 80% yield, further increasing the yield to 99%. N-Boc piperidine acetic acid 183 was coupled to 182 under conventional amide bond formation conditions. Subsequent removal of the Boc protecting group and urea bond formation using N-methylpyrrolidone (NMP) and urea ultimately afforded lonafarnib (XXIV).

target

FT

storage

Store at -20°C

LONAFARNIB Preparation Products And Raw materials

Raw materials

Preparation Products

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LONAFARNIB Suppliers

China 158 India 3 South Korea 1 United Kingdom 1 United States 19 Global 182

SuZhou GoodChemTech Co., Ltd

Tel: 18136139868; 18136139868
Email: jinlun@goodchemtech.cn
Country: China
ProdList: 284
Advantage: 58

Shanghai Boyle Chemical Co., Ltd.

Tel
Fax: 86-21-57758967
Email: sales@boylechem.com
Country: China
ProdList: 2922
Advantage: 55

J & K SCIENTIFIC LTD.

Tel: 18210857532; 18210857532
Fax: 86-10-82849933
Email: jkinfo@jkchemical.com
Country: China
ProdList: 96815
Advantage: 76

Chembest Research Laboratories Limited

Tel: +86-21-20908456
Fax: 021-58180499
Email: sales@BioChemBest.com
Country: China
ProdList: 6003
Advantage: 61

Adamas Reagent, Ltd.

Tel: 400-6009262 16621234537
Fax: 021-64823266
Email: chenyj@titansci.com
Country: China
ProdList: 14101
Advantage: 59

Chemsky（shanghai）International Co.,Ltd.

Tel: 021-50135380
Email: shchemsky@sina.com
Country: China
ProdList: 32321
Advantage: 50

Dalian Meilun Biotech Co., Ltd.

Tel: 0411-62910999 13889544652
Email: sales@meilune.com
Country: China
ProdList: 4747
Advantage: 58

Beijing HuaMeiHuLiBiological Chemical

Tel: 010-56205725
Fax: 010-65763397
Email: waley188@sohu.com
Country: China
ProdList: 12335
Advantage: 58

NCE Biomedical Co.,Ltd.

Tel: 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax: +86-27-87599188
Country: China
ProdList: 1493
Advantage: 55

Jiangsu Aikon Biopharmaceutical R&D co.,Ltd.

Tel: 025-66113011 17798518460
Fax: (1)02557626880
Email: cfzhang@aikonchem.com
Country: China
ProdList: 19913
Advantage: 55

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View Lastest Price from LONAFARNIB manufacturers

Career Henan Chemical Co

Product: LONAFARNIB 193275-84-2
Price: US $2.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100kg
Release date: 2018-12-24

193275-84-2, LONAFARNIBRelated Search:

Everolimus Selumetinib MK-2206 2HCl Tipifarnib Ibrutinib PLX4032 PIPERIDINE, 4-[(2-METHYLPHENYL)METHYL]-, HYDROCHLORIDE 1-Bromo-4-chloro-2-methylbenzene LONAFARNIB 4-(2-METHYL-BENZYL)-PIPERIDINE Pyridine, 3-bromo-5-ethyl- (9CI) 1-(2-PIPERIDIN-4-YL-ETHYL)-PIPERIDINE 4-(4-CHLOROBENZYL)PIPERIDINE

LONAFARNIB

SARASAR; SCH 66336; SCH66336; SCH-66336

4-(2-(4-((R)-3,10-dibroMo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)cyclohexyl)-2-oxoethyl)piperidine-1-carboxaMide

Lonafarnib (SCH66336)

1-Piperidinecarboxamide, 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)-

4-(2-(4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo-(5,6)-cyclohepta(1,2-B)-pyridin-11(R)-yl)-1-piperidinyl)-2-oxo-ethyl)-1-piperidinecarboxamide

Lonafarnib [usan]

Sarasar

Sch 66336

Sch66336

Unii-iow153004f

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-

1-PiperidinecarboxaMide, 4-[2-[4-[(11R)-3,10-dibroMo-8-chloro-6

LonafarMib

(R)-4-(2-(4-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl)-2-oxoethyl)piperidine-1-carboxamide

EOS-61911

( )4-(2-(4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo(5,6)cyclohepta (1,2-b)pyridin-11-yl)-1-piperidinyl)-2-oxoethyl)-1-piperidinecarboxami de

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

SCH-066336

LONAFARNIB USP/EP/BP

Lonafarnib Sarasar SCH 66336

Valine Impurity 114

Lonafarnib, 10 mM in DMSO

Lonafarnib (SCH66336) ，S2797

193275-84-2

Inhibitor

Aromatics

Heterocycles

Inhibitors

Intermediates & Fine Chemicals

Pharmaceuticals

APIs