产品说明书

RG13022

Print
Chemical Structure| 136831-48-6 同义名 : Tyrphostin RG13022
CAS号 : 136831-48-6
货号 : A646643
分子式 : C16H14N2O2
纯度 : 99%+
分子量 : 266.295
MDL号 : MFCD00236444
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：
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].
实验方案
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
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