Tipifarnib

Bezeichnung:Tipifarnib

CAS-Nr192185-72-1

Englisch Name:Tipifarnib

CBNumberCB61011759

SummenformelC27H22Cl2N4O

Molgewicht489.4

MOL-Datei192185-72-1.mol

Tipifarnib physikalisch-chemischer Eigenschaften

Schmelzpunkt	211-213°C (dec.)
Siedepunkt	681.7±55.0 °C(Predicted)
Dichte	1.33±0.1 g/cm3(Predicted)
storage temp.	-20°C
Löslichkeit	Chloroform (Slightly), Methanol (Slightly)
pka	7.20±0.10(Predicted)
Aggregatzustand	powder
Farbe	white to beige
Optische Aktivität	[α]/D 17 to 24°, c = 1 in methanol

Sicherheit

HS Code

2933790090

Gefahreninformationscode (GHS)

Tipifarnib Chemische Eigenschaften,Einsatz,Produktion Methoden

Chemische Eigenschaften
Off-White to Pale Beige Solid
Verwenden
A farnesyltransferase inhibitor. Sensitizes human multiple myeloma cell to proteasome inhibition by blocking degradation of bortezomib(B675700)-induced aggresomes. Also shown to inhibit the growth of myeloid leukemia cell lines and primary leukemia cells by inducing apoptosis and cell-cycle blockage when combined with rapamycin(R124000).
Definition
ChEBI: Tipifarnib is a quinolone that is 1-methylquinolin-2-one which carries a 3-chlorophenyl and an amino(4-chlorophenyl)(1-methyl-imidazol-5-yl)methyl groups at the 4 and 6 positions, respectively (the R-isomer). It has a role as an antineoplastic agent, an EC 2.5.1.58 (protein farnesyltransferase) inhibitor and an apoptosis inducer. It is a quinolone, a member of monochlorobenzenes, a member of imidazoles and a primary amino compound.
Allgemeine Beschreibung
Pre-clinical studies show that tipifarnib has antiproliferative effects on pancreatic cancer cell lines at clinically relevant concentrations (concentration that inhibits 50% growth [IC50] from 9.5 to 500?nmol/L). It also exhibits marked growth retardation and antiangiogenic effects in a pancreatic cancer xenograft model.
Biologische Aktivität
tipifarnib (also known as zarnestra or r115777), an orally bioavailable quinolone analog of imidazole heterocyclics, is a potent and specific nonpeptidomimetic competitive inhibitor of farnesyltransferase (ftase), an enezyme mediating post-translational farnesylation of multiple protein substrates involved in tumor cell proliferation. it has demonstrated inhibition of growth and proliferation of a broad range of human tumor models (either wild-type or mutated ras) via cytostatic rather than cytotoxic activity both in vitro and in vivo. it cell-type dependently induces apoptosis in some neoplastic cell lineages other than acute myeloid leukemia (aml), including multiple myeloma (mm) cell lines and mm cultures from patients.p.k. epling-burnett and thomas p. loughran jr. suppression of farnesyltransferase activity in acute myeloid leukemia and myelodysplastic syndrome: current understanding and recommended use of tipifarnib. expert opin investig drugs. 2010; 19(5): 689-698jean-pierre armand, alan k. burnett, johannes drach, jean-luc harousseau, bob lowenberg and jesus san miguel. the emerging role of targeted therapy for hematologic malignancies: update on bortezomib and tipifarnib. the oncologist 2007, 12:281-290elzbieta izbicka, david campos, gilbert carrizales and amita patnaik. biomarkers of anticancer activity of r115777 (tipifarnib, zarnestra) in human breast cancer models in vitro. anticancer research 2005; 25: 3215-3224
Biochem/physiol Actions
Tipifarnib (R115777) is an orally active and potent farnesyltransferase (FTase) inhibitor that exhibits potent anti-tumorigenic effects. Tipifarnib mechanism of action is not fully understand.
target
FTase

Tipifarnib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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