Tipifarnib
- CAS No.
- 192185-72-1
- Chemical Name:
- Tipifarnib
- Synonyms
- R115777;CS-2330;IND 58359;Zarnestra;ipifarnib;TIPIFARNIB;(R)-(+)-R 115777;Tipifarnib(R115777);TIPIFARNIB ZARNESTRA;Tipifarnib USP/EP/BP
- CBNumber:
- CB61011759
- Molecular Formula:
- C27H22Cl2N4O
- Molecular Weight:
- 489.4
- MDL Number:
- MFCD07772347
- MOL File:
- 192185-72-1.mol
- MSDS File:
- SDS
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 |
NCI Dictionary of Cancer Terms | R115777; tipifarnib; Zarnestra |
FDA UNII | MAT637500A |
NCI Drug Dictionary | tipifarnib |
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
---|---|
Signal word | Warning |
Hazard statements | H315-H319-H335 |
Precautionary statements | P305+P351+P338 |
HS Code | 2933790090 |
Tipifarnib price More Price(47)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | SML1668 | Tipifarnib ≥98% (HPLC) | 192185-72-1 | 5MG | $131 | 2023-06-20 | Buy |
Sigma-Aldrich | SML1668 | Tipifarnib ≥98% (HPLC) | 192185-72-1 | 25MG | $530 | 2023-06-20 | Buy |
Cayman Chemical | 11747 | Tipifarnib ≥98% | 192185-72-1 | 1mg | $44 | 2024-03-01 | Buy |
Cayman Chemical | 11747 | Tipifarnib ≥98% | 192185-72-1 | 5mg | $118 | 2024-03-01 | Buy |
Cayman Chemical | 11747 | Tipifarnib ≥98% | 192185-72-1 | 10mg | $214 | 2024-03-01 | Buy |
Tipifarnib Chemical Properties,Uses,Production
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).
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
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 | sales@capotchem.com | China | 29798 | 60 |
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32760 | 60 |
career henan chemical co | +86-0371-86658258 +8613203830695 | sales@coreychem.com | China | 29900 | 58 |
Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 | sales@chemdad.com | China | 39916 | 58 |
CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49391 | 58 |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 26114 | 58 |
Chemia Biotechnology(Shanghai) Co., Ltd | +8613816753574 | info@chemia-pharm.com | CHINA | 311 | 58 |
Finetech Industry Limited | +86-27-87465837 +8618971612321 | info@finetechnology-ind.com | China | 9626 | 58 |
Hefei Hirisun Pharmatech Co., Ltd | +8615056975894 | shawn@hirisunpharm.com | CHINA | 9923 | 58 |
View Lastest Price from Tipifarnib manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
---|---|---|---|---|---|---|---|---|
2019-07-06 | Tipifarnib
192185-72-1
|
US $2.00 / kg | 1kg | 99% | 100kg | Career Henan Chemical Co |
- Tipifarnib
192185-72-1
- US $2.00 / kg
- 99%
- Career Henan Chemical Co