LONAFARNIB

Bezeichnung:LONAFARNIB

CAS-Nr193275-84-2

Englisch Name:LONAFARNIB

CBNumberCB31011743

SummenformelC27H31Br2ClN4O2

Molgewicht638.82

MOL-Datei193275-84-2.mol

LONAFARNIB physikalisch-chemischer Eigenschaften

Schmelzpunkt	214.5-215.9° (monohydrate); mp 222-223°
alpha	D25 = +49.1° (c = 0.21 in methanol)
Siedepunkt	710.4±70.0 °C(Predicted)
Dichte	1.536
storage temp.	-20°C
Löslichkeit	Chloroform (Slightly), Methanol (Slightly)
pka	15.76±0.40(Predicted)
Aggregatzustand	powder
Farbe	white to beige

Gefahreninformationscode (GHS)

LONAFARNIB Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
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
Verwenden
Chemotherapeutic (farnesyl transfer ase inhibitor).
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.
Allgemeine Beschreibung
Lonafarnib (SCH66336) is a farnesyl transferase inhibitor (FTI). K- and N-Ras are substrates of farnesyl transferase.
Biologische Aktivität
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.
Nebenwirkungen
- vomiting
- diarrhea
- nausea
- stomach pain
- constipation
- gas
- decreased appetite
- decreased weight
target
FT
Lager
Store at -20°C

LONAFARNIB Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

193275-84-2, LONAFARNIB Verwandte Suche:

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