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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
$134
Updated
2024/03/01
Sigma-Aldrich
Product number
SML1457
Product name
Lonafarnib
Purity
≥98% (HPLC)
Packaging
25MG
Price
$462
Updated
2024/03/01
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

target

FT

storage

Store at -20°C

LONAFARNIB Preparation Products And Raw materials

Raw materials

Preparation Products

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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:


  • 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
  • 193275-84-2
  • Inhibitor
  • Aromatics
  • Heterocycles
  • Inhibitors
  • Intermediates & Fine Chemicals
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