Tipifarnib (Zarnestra)|192185-72-1|(替吡法尼; IND 58359; R115777)-陌孚医药/Medlife

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Tipifarnib (Zarnestra) (Synonyms: 替吡法尼; IND 58359; R115777)

目录号: PC12469 纯度: ≥98%

CAS No. :192185-72-1

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中文名称

Tipifarnib (Zarnestra)

中文别名

替吡法尼;(R)-6-(氨基(4-氯苯基)(1-甲基-1H-咪唑-5-基)甲基)-4-(3-氯苯基)-1-甲基-2(1H)-喹啉酮;溴甲基苯基砜

英文名称

Tipifarnib (Zarnestra)

英文别名

Tipifarnib;(R)-6-(Amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl)-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone;6-[(R)-amino-(4-chlorophenyl)-(3-methylimidazol-4-yl)methyl]-4-(3-chlorophenyl)-1-methylquinolin-2-one;LM 22A4;Tipifarnib (Zarnestra);IND 58359;IND-58359;R115777;R-115777;Zarnestra;(R)-(+)-R 115777;6-[(R)-Amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone;Tipifarnib(R115777);TIPIFARNIB ZARNESTRA;Tipifarnib(Zarnestra,NSC-702818, R-115777);(R)-6-(amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl)-4-(3-chlorophenyl)-1-methylquinolin-2(1H)-one;Tipifarnib (IND 58359

Cas No.

192185-72-1

分子式

C₂₇H₂₂Cl₂N₄O

分子量

489.40

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Tipifarnib (IND 58359) binds to and inhibits farnesyltransferase (FTase) with an IC₅₀ of 0.86 nM. Antineoplastic activity.

性状

Solid

IC50 & Target[1][2]

IC50: 0.86 nM (FTase)

体外研究(In Vitro)

Tipifarnib inhibits the growth of H-Ras-transformed NIH 3T3 cells with an impressive IC₅₀ value of 1.7 nM .
Tipifarnib is a potent inhibitor of Trypanosoma Cruzi with the ED₅₀ of 4 nM.
Combining Tipifarnib with 10 nM 4-OH-ICI 47699 in the presence of E2 reduces the IC₅₀ 8-fold from 400 to 50 nM.
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.
Tipifarnib shows inhibition of cell growth or angiogenesis, and induction of apoptosis in aggressive prostate cancer (PCa).
Tipifarnib shows a significant decrease in the concentration of exosomes in C4-2B cells both at 0.25 and 1?μM as well as in the PC-3 cells at 0.25?μM for 48?hours.
Tipifarnib (1?μM) significantly inhibits the protein concentration of Alix, nSMase2, and Rab27a in C4-2B cells.
Tipifarnib (0.25 μM) significantly inhibits the activation of p-ERK (downstream effector molecule of the Ras/Raf/ERK signaling pathway) but not total ERK in C4-2B and PC-3 cells but not in the normal RWPE-1 cells.
Tipifarnib (0-250?nM) causes a dose-dependent decrease in Alix, nSMase2, and Rab27a in both C4-2B and PC-3 cells, but not in the RWPE-1 cells, Tipifarnib has the potential to be a potent inhibitor of exosome biogenesis and/or secretion.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Combined therapy with ICI 47699 and Tipifarnib (50 mg/kg, p.o.) produces greater tumor growth inhibition when compared with either drug alone. E2 deprivation and Tipifarnib in combination results in greater growth inhibition than either E2 deprivation or Tipifarnib alone. The combination of ICI 47699 and Tipifarnib results in significantly lower Ki-67 compared with either ICI 47699 or Tipifarnib alone. Tipifarnib alone also reduces the CTI compared with control. The combination of ICI 47699 and Tipifarnib or Tipifarnib 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Devendra S Puntambekar, et al. Inhibition of farnesyltransferase: a rational approach to treat cancer? J Enzyme Inhib Med Chem. 2007 Apr;22(2):127-40. [Information]

[2]. Martin LA, et al. The farnesyltransferase inhibitor R115777 (tipifarnib) in combination with ICI 47699 acts synergistically to inhibit MCF-7 breast cancer cell proliferation and cell cycle progression 体外研究 and in vivo. Mol Cancer Ther. 2007 Sep;6(9):2 [Information]

[3]. End DW, et al. Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and 体外研究. Cancer Res. 2001 Jan 1;61(1):131-7 [Information]

[4]. Amrita Datta, et al. High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. Sci Rep. 2018 May 25;8(1):8161. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (204.33 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 20% HP-β-CD/10 mM citrate pH 2.0
Solubility: 10 mg/mL (20.43 mM); Clear solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.43 mg/mL (2.92 mM); Clear solution

此方案可获得 ≥ 1.43 mg/mL (2.92 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 1.43 mg/mL (2.92 mM); Suspended solution; Need ultrasonic

此方案可获得 1.43 mg/mL (2.92 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.43 mg/mL (2.92 mM); Clear solution

此方案可获得 ≥ 1.43 mg/mL (2.92 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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