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XRP44X
目录号: PC11811 纯度: ≥98%
CAS No. :729605-21-4
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中文名称
XRP44X
中文别名
[4-(3-氯苯基)哌嗪-1-基](5-甲基-2-苯基-2H-吡唑-3-基)甲酮
英文名称
XRP44X
英文别名
Piperazine,1-(3-chlorophenyl)-4-[(3-methyl-1-phenyl-1H-pyrazol-5-yl)carbonyl]-;XRP44X;(4-(3-Chlorophenyl)piperazin-1-yl)(3-methyl-1-phenyl-1H-pyrazol-5-yl)methanone;[4-(3-chlorophenyl)piperazin-1-yl]-(5-methyl-2-phenylpyrazol-3-yl)methanone;[4-(3-Chlorophenyl)-1-piperazinyl](3-methyl-1-phenyl-1H-pyrazol-5-yl)-methanone;1-(3-Chlorophenyl)-4-((3-methyl-1-phenyl-1H-pyrazol-5-yl)carbonyl)piperazine;1-(3-CHLOROPHENYL)-4-[(3-METHYL-1-PHENYL-1H-PYRAZOL-5-YL)CARBONYL]PIPERAZINE;MLS006010688;NPHPNBGYPKBDDB-UHFFFAOYSA-N;XR
Cas No.
729605-21-4
分子式
C21H21ClN4O
分子量
380.87
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

XRP44X inhibits Ras-induced transcription activation with the IC50 of 10 nM. XRP44X inhibits activation of the Ras-Erk-1/2 pathway by FGF-2. XRP44X is an inhibitor of Ras/Erk activation of Elk3 that also affects microtubules.

性状

Solid

IC50 & Target[1][2]

Ras

10 nM (IC50)

体外研究(In Vitro)

XRP44X is an indirect inhibitor of Net phosphorylation that acts upstream from Erk-1/2 activation. XRP44X inhibits luciferase activity with the IC50 of~10 nM.
XRP44X (10 nM) inhibits cell growth of HUVEC, NIH3T3, HCT-116, and NIH3T3–Ki-Ras cells.
XRP44X (100 nM) inhibits phosphorylation of Mek-1/2 and Raf-1.

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

Cell Proliferation Assay

Cell Line: HUVEC, NIH3T3, HCT-116, and NIH3T3-Ki-Ras cells
Concentration: 10 nM
Incubation Time: 24, 48, 72, 96 hours
Result: Inhibited HUVEC, HCT 116,NIH3T3, and NIH3T3-RAS cells proliferation with IC50s of 2.2±0.5 nM, 2.3±0.5 nM, 4±0.5 nM, and 2.3±0.5 nM, respectively.
Inhibited the growth of immortalized mouse fibroblasts.

Western Blot Analysis

Cell Line: HUVEC cells
Concentration: 100 nM
Incubation Time: Pretreated for 90 minutes
Result: Inhibited phosphorylation of Rsk-1.
Inhibited phosphorylation of Erk-1/2 on sites required for its activation without affecting overall levels of Erk-1/2.
体内研究(In Vivo)

XRP44X may have therapeutic potential for refractory asthma.
XRP44X, an inhibitor of Ras/Erk activation of the transcription factor Elk3, inhibits tumor growth and metastasis in mice. XRP44X inhibits tumor growth and metastasis in nude mice. XRP44X decreases the growth of tumours and the formation of metastases in nude mice.

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

Animal Model: Male nude mice (BALB/c nu/nu)
Dosage: 1 mg/kg
Administration: Intraperitoneal injection; treated daily for 6 days
Result: Inhibited cell tumor formation by xenografts in nude mice.
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
参考文献
溶解度数据
体外研究: 

DMSO : 50 mg/mL (131.28 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 2.6256 mL 13.1278 mL 26.2557 mL
5 mM 0.5251 mL 2.6256 mL 5.2511 mL
10 mM 0.2626 mL 1.3128 mL 2.6256 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。

搜索质检报告(COA)

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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