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Description: Potent farnesyltransferase inhibitor; orally bioavailable
Chemical Name: 6-[(R)-Amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl}-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone
Purity: ≥98% (HPLC)
Biological Activity for Tipifarnib
Tipifarnib is a potent farnesyltransferase inhibitor. Inhibits farnesylation of lamin B and K-RasB peptide substrates (IC50 values are 0.86 and 7.9 nM, respectively). Inhibits tumor growth in vitro and in vivo. Cell penetrant and orally bioavailable.
Technical Data for Tipifarnib
| M. Wt | 489.4 |
| Formula | C27H22Cl2N4O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 192185-72-1 |
| PubChem ID | 159324 |
| InChI Key | PLHJCIYEEKOWNM-HHHXNRCGSA-N |
| Smiles | CN1C=NC=C1[C@@](C2=CC=C(C=C2)Cl)(C3=CC=C4N(C(C=C(C4=C3)C5=CC(Cl)=CC=C5)=O)C)N |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Tipifarnib
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 48.94 | 100 | |
| ethanol | 9.79 | 20 |
Preparing Stock Solutions for Tipifarnib
The following data is based on the product molecular weight 489.4. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.04 mL | 10.22 mL | 20.43 mL |
| 5 mM | 0.41 mL | 2.04 mL | 4.09 mL |
| 10 mM | 0.2 mL | 1.02 mL | 2.04 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.41 mL |
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Product Datasheets for Tipifarnib
References for Tipifarnib
References are publications that support the biological activity of the product.
End et al (2001) Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro. Cancer Res. 61 131 PMID: 11196150
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Keywords: Tipifarnib, Tipifarnib supplier, Potent, farnesyltransferase, inhibitors, inhibits, antitumor, cell, penetrant, orally, bioavailable, Protein, Prenyltransferases, Post-translational, Modifications, 6410, Tocris Bioscience
Citations for Tipifarnib
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Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
- Cancer Metabolism
- Epigenetics in Cancer
- Receptor Signaling
- Cell Cycle and DNA Damage Repair
- Angiogenesis
- Invasion and Metastasis