- Tipifarnib
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- $2.00 / 1kg
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2019-07-06
- CAS:192185-72-1
- Min. Order: 1kg
- Purity: 99%
- Supply Ability: 100kg
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| | Tipifarnib Basic information |
| | Tipifarnib Chemical Properties |
| Melting point | 211-213°C (dec.) | | Boiling point | 681.7±55.0 °C(Predicted) | | density | 1.33±0.1 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | Chloroform (Slightly), Methanol (Slightly) | | pka | 7.20±0.10(Predicted) | | form | powder | | color | white to beige | | optical activity | [α]/D 17 to 24°, c = 1 in methanol |
| | Tipifarnib Usage And Synthesis |
| Chemical Properties | Off-White to Pale Beige Solid | | Uses | 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). | | Uses | 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. | | General Description | 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. | | Biological Activity | 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 Preparation Products And Raw materials |
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