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
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
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.
N-Bromosuccinimide Price
- Product number
- SML1457
- Product name
- Lonafarnib
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $134
- Updated
- 2024/03/01
- Product number
- SML1457
- Product name
- Lonafarnib
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $462
- Updated
- 2024/03/01
- Product number
- 11746
- Product name
- Lonafarnib
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $33
- Updated
- 2024/03/01
- Product number
- 11746
- Product name
- Lonafarnib
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $112
- Updated
- 2024/03/01
- Product number
- 11746
- Product name
- Lonafarnib
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $143
- Updated
- 2024/03/01
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
- Product
- LONAFARNIB 193275-84-2
- Price
- US $2.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 100kg
- Release date
- 2018-12-24