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Tipifarnib

Catalog No. T6271 CAS 192185-72-1

Synonyms: R115777, Zarnestra, IND 58359

Tipifarnib (IND 58359) is a nonpeptidomimetic quinolinone with potential antineoplastic activity. Tipifarnib binds to and inhibits the enzyme farnesyl protein transferase, an enzyme involved in protein processing (farnesylation) for signal transduction. By inhibiting the farnesylation of proteins, this agent prevents the activation of Ras oncogenes, inhibits cell growth, induces apoptosis, and inhibits angiogenesis.

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Tipifarnib, CAS 192185-72-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
2 mg	In stock	$ 48.00
5 mg	In stock	$ 77.00
10 mg	In stock	$ 133.00
25 mg	In stock	$ 253.00
50 mg	In stock	$ 458.00
1 mL * 10 mM (in DMSO)	In stock	$ 84.00

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Purity: 99.22%

Purity: 97.23%

Purity: 97.1%

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Description	Tipifarnib (IND 58359) is a nonpeptidomimetic quinolinone with potential antineoplastic activity. Tipifarnib binds to and inhibits the enzyme farnesyl protein transferase, an enzyme involved in protein processing (farnesylation) for signal transduction. By inhibiting the farnesylation of proteins, this agent prevents the activation of Ras oncogenes, inhibits cell growth, induces apoptosis, and inhibits angiogenesis.
Targets&IC50	FTase:0.6 nM
In vitro	Using Tipifarnib 5 μM for 72 hours, the percentage of apoptotic cells is significantly higher in drug-treated compared to DMSO-treated LGL T-cells. Using T-cells from healthy donors, Tipifarnib reduces the percentage of IFNγ-positive cells in a time-dependent manner. Tipifarnib reduces the amount of activated Ras in precipitates compared to DMSO. [2] Tipifarnib exerts selective in vitro toxicity against clonal MDS hematopoiesis at concentrations less than 10 nM the effect being more prominent in white cell progenitors. This action is not due to apoptosis induction as both normal and MDS progenitors displays equivalent DiOC3 and annexin V expression up to 72 hours after exposure to Tipifarnib. [3] Combining Tipifarnib with 10 nM 4-OH-tamoxifen in the presence of E2 reduces the IC50 8-fold from 400 to 50 nM. [4] Tipifarnib induces apoptosis in U937 cells. [5] In addition, Tipifarnib inhibits isolated human farnesyltransferase for a lamin B peptide and for the K-RasB peptide with IC50 of 0.86 nM and 7.9 nM, respectively. [6]
In vivo	Ki-67 is lower in the tumors treated with E2 withdrawal plus R115777 compared with E2 withdrawal alone. The combination of tamoxifen and R115777 results in significantly lower Ki-67 compared with either tamoxifen or R115777 alone (mean of 5% versus 16.9% and 67.3%, respectively). [4] In contrast, no significant difference in apoptotic scores is seen between the treatment groups. R115777 alone also reduces the CTI compared with control. The combination of tamoxifen and R115777 or R115777 coupled with E2 withdrawal is most effective at lowering the CTI (0.8 and 0.7, respectively), which may account for the decrease in tumor volume. [4]
Cell Research	MACS-selected CD34+ cells are seeded in Methocult 4435 'complete' 1% bovine serum albumin, 3 U/mL recombinant human (rh) erythropoietin, 0.1 mM 2-mercaptoethanol, 2 mM L-glutamine and the following cytokines: 50 ng/mL rh stem cell factor, 20 ng/mL rh GM-CSF, 20 ng/mL rh IL-3, 20 ng/mL rh IL-6 and 20 ng/mL h G-CSF. DMSO or Tipifarnib is added at the concentrations of 2.5, 10, 25 and 50 nM at day 1. All cultures are performed in duplicates and the numbers of colonies are scored after 14 days of incubation at 37 °C in a humidified incubator containing 5% CO2</sub(Only for Reference)

Synonyms	R115777, Zarnestra, IND 58359
Molecular Weight	489.4
Formula	C27H22Cl2N4O
CAS No.	192185-72-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 48.9 mg/mL (100 mM)

Ethanol: 9.8 mg/mL (20 mM)

References and Literature

1. Margolin KA, et al. Clin Cancer Res. 2012, 18(4), 1129-1137. 2. Bai F, et al. Cancer Immunol Immunother. 2012, 61(4), 523-533. 3. Kotsianidis I, et al. Acta Haematol. 2008, 120(1), 51-56. 4. Martin LA, et al. Mol Cancer Ther. 2007, 6(9), 2458-2467. 5. Krzykowska-Petitjean K, et al. J Cancer Res Clin Oncol. 2012, 138(3), 537-544.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Active Compound Library Pediatric Drug Library Anti-Liver Cancer Compound Library Anti-Pancreatic Cancer Compound Library Angiogenesis related Compound Library Preclinical Compound Library

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Keywords

Tipifarnib 192185-72-1 Metabolism Transferase Inhibitor Farnesyl Transferase inhibit R115777 Zarnestra R-115777 R 115777 IND-58359 Ftase IND 58359 IND58359 inhibitor

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