|3-(3,4-二甲氧基苯基)-2-(吡啶-3-基)丙烯腈|CsnPharm

CAS No.: 136831-48-6

RG13022 Catalog No. CSN25272

Synonyms: Tyrphostin RG13022

RG-13022 significantly inhibited EGF-stimulated autophosphorylation of its receptor in two breast cancer cell lines that have abundant, although not amplified, EGF receptor content (MDA-231 and T47D).RG-13022 suppressed not only EGF-stimulated cancer cell proliferation in vitro but also tumor growth in nude mice. RG-13022 also increased the life span of these tumor-bearing nude mice.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.7552 mL
- 18.7762 mL
- 37.5524 mL
- 5 mM
- 0.7510 mL
- 3.7552 mL
- 7.5105 mL
- 10 mM
- 0.3755 mL
- 1.8776 mL
- 3.7552 mL

技术信息

CAS号

136831-48-6

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H14N2O2

运输

蓝冰

分子量

266.29

别名

Tyrphostin RG13022

溶解度

DMSO	53.0 mg/mL (199.0 mM)
Water	Insoluble
Ethanol	5.0 mg/mL (18.8 mM)

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

RG13022 Catalog No. CSN25272

靶点选择性

请登录您的专属账户

确认信息