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Tipifarnib (Zarnestra) Sale

(Synonyms: 替吡法尼; IND 58359; R115777) 目录号 : GC15442

A farnesyltransferase inhibitor with antitumor activity

Tipifarnib (Zarnestra) Chemical Structure

Cas No.:192185-72-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,400.00
现货
5mg
¥1,080.00
现货
25mg
¥3,330.00
现货
100mg
¥8,910.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment: [1]

Cell lines

Human leukemia cell line THP-1

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

100 ng/ml LPS plus 2 μM tipifarnib. 6 time points (0, 10, 20, 30, 40 and 50h)

Applications

Tipifarnib showed significant inhibition of the cytokine/ MMP-9 production as early as 20 h for MCP-1 and IL-6 and 30 h for IL-1β and MMP-9. Tipifarnib showed no significant inhibition of IL-8 production.

Animal experiment : [1]

Animal models

Female BALB/c mice (6–7 weeks old)

Dosage form

Tipifarnib was dissolved in 20% cyclodextran, and 50 mg/kg was orally administered to mice at 24, 17, and 1 h before intraperitoneal injection of 20 μg of LPS per mouse, 1 mg/kg.

Applications

After treatment of 2h, tipifarnib significantly inhibited LPS-induced TNF-α production and inhibited 50% of MIP-1α and MCP-1 production. After 3h, tipifarnib inhibited about 50% of IL-6 production and almost complete inhibition of IL-1β production. IL12-p40 and -p70 induction by LPS was also inhibited by tipifarnib at 3 h, whereas IL-10 was not significantly changed at both time points. No effects of tipifarnib on LPS-induced KC were observed, consistent with in vitro results for IL-8.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Xue X, Lai K T A, Huang J F, et al. Anti-inflammatory activity in vitro and in vivo of the protein farnesyltransferase inhibitor tipifarnib. Journal of Pharmacology and Experimental Therapeutics, 2006, 317(1): 53-60.

产品描述

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.

Reference

[1].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): 689-698
[2].Jean-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, 12:281-290
[3].Elzbieta 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

Chemical Properties

Cas No. 192185-72-1 SDF
别名 替吡法尼; IND 58359; R115777
化学名 6-[(R)-amino-(4-chlorophenyl)-(3-methylimidazol-4-yl)methyl]-4-(3-chlorophenyl)-1-methylquinolin-2-one
Canonical SMILES CN1C=NC=C1C(C2=CC=C(C=C2)Cl)(C3=CC4=C(C=C3)N(C(=O)C=C4C5=CC(=CC=C5)Cl)C)N
分子式 C27H22Cl2N4O 分子量 489.4
溶解度 ≥ 8.16 mg/mL in DMSO, ≥ 9.16 mg/mL in EtOH with ultrasonic 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.0433 mL 10.2166 mL 20.4332 mL
5 mM 0.4087 mL 2.0433 mL 4.0866 mL
10 mM 0.2043 mL 1.0217 mL 2.0433 mL
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