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RG13022 {[allProObj[0].p_purity_real_show]}

货号:A646643 同义名: Tyrphostin RG13022

RG13022是一种酪氨酸激酶抑制剂,主要靶向表皮生长因子受体(EGFR)。在无细胞实验中,RG13022以4 μM的IC₅₀值抑制EGFR的自身磷酸化。此外,RG13022能够剂量依赖性地抑制EGF刺激的HER 14细胞的集落形成和DNA合成,IC₅₀值分别为1 μM和3 μM。

RG13022 化学结构 CAS号:136831-48-6
RG13022 化学结构
CAS号:136831-48-6
RG13022 3D分子结构
CAS号:136831-48-6
RG13022 化学结构 CAS号:136831-48-6
RG13022 3D分子结构 CAS号:136831-48-6
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RG13022 纯度/质量文件 产品仅供科研

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RG13022 生物活性

靶点
  • EGFR/ErbB1

    EGFR, IC50:4 μM

描述 Growth factor receptors with tyrosine kinase activity mediate paracrine and autocrine growth regulation of normal and malignant cells. The epidermal growth factor receptor (EGF-R) is a tyrosine kinase transmembrane protein that is overexpressed by many epithelial malignancies[1]. RG13022, a tyrosine kinase inhibitor, inhibits the autophosphorylation reaction of the EGF-R in immunoprecipitates with an IC50 of 4 μM. RG-13022 inhibits DNA synthesis and colony formation by HER 14 cells, which are stimulated by 50 ng/mL EGF, in a dose-dependent manner. The IC50s for RG-13022 are 3 μM and 1 μM for HER 14 DNA synthesis and HER 14 colony formation, respectively. RG-13022 also suppresses DNA synthesis and colony formation by EGF-stimulated MH-85 cells in a dose-dependent manner. The IC50s for RG-13022 on MH-85 cells are 1.5 μM and 7 μM for DNA synthesis and colony formation, respectively. Nude mice implanted with MH-85 tumors manifested profound hypercalcemia, cachexia, and leukocytosis as the tumor grew. RG-13022 (400 μg/mouse/day) significantly inhibits MH-85 tumor growth in Nude Mice. Because of slower tumor growth, MH-85 tumor-bearing animals receiving injections of RG-13022 show less cachexia and hypercalcemia, eat more food, and are more active than untreated MH-85 tumor-bearing animals. RG-13022 prolongs the life span of MH-85 tumor-bearing animals as a result of suppression of tumor growth. Moreover, administration of mAb108 i.p. (1 mg/mouse/day) at 1, 5, and 10 days after MH-85 inoculation of RG-13022 (400 μg/mouse/day) for 14 days profoundly inhibits MH-85 growth in nude mice[2].

RG13022 参考文献

[1]Sion-Vardy N, Vardy D, Rodeck U, Kari C, Levin RM, Malkowicz SB. Antiproliferative effects of tyrosine kinase inhibitors (tyrphostins) on human bladder and renal carcinoma cells. J Surg Res. 1995;59(6):675-680

[2]Yoneda T, Lyall RM, Alsina MM, et al. The antiproliferative effects of tyrosine kinase inhibitors tyrphostins on a human squamous cell carcinoma in vitro and in nude mice. Cancer Res. 1991;51(16):4430-4435

RG13022 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.76mL

0.75mL

0.38mL

18.78mL

3.76mL

1.88mL

37.55mL

7.51mL

3.76mL

RG13022 技术信息

CAS号136831-48-6
分子式C16H14N2O2
分子量 266.295
别名 Tyrphostin RG13022
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Sealed in dry,2-8°C

溶解方案

DMSO: 105 mg/mL(394.3 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案一
方案二
动物实验配方
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