Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tyrphostin AG 879 (AG 879) 是一种抑制TrKA 磷酸化的酪氨酸激酶抑制剂,IC50为 10 μM。它还是一种选择性ErbB2酪氨酸激酶抑制剂,IC50为 1 μM,具有抗癌活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 233 | 现货 | ||
5 mg | ¥ 413 | 现货 | ||
10 mg | ¥ 663 | 现货 | ||
25 mg | ¥ 1,580 | 现货 | ||
50 mg | ¥ 2,660 | 现货 | ||
100 mg | ¥ 3,930 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 455 | 现货 |
产品描述 | Tyrphostin AG 879 (AG 879) effectively inhibits HER2/ErbB2 (IC50: 1 μM), 100- and 500-fold higher selective to ErbB2 than EGFR and PDGFR. |
靶点活性 | HER2/ErbB2:1 μM |
体外活性 | AG879 inhibits growth of FET6αS26X cells in a concentration-dependent manner. [1] AG879(10 nM) blocks the activation of PAK1 and suppresses RAS-induced malignant transformation of NIH 3T3 cells. AG879(<1 μM) inhibits the Tyr-phosphorylation of ERK and its association with PAK1 in v-Ha-RAS-transformed NIH 3T3 fibroblasts. [2] AG 879 dose-dependently reduce MCF-7 cell numbers and show already a significant effect at 0.4 mM through inhibiting DNA synthesis and mitotic. AG 879(<20 μM) inhibits activation of ERK-1/2 in MCF-7 cell. AG 879(5 μM) decreases expression of Hsp90 client proteins RAF-1 and HER-2. [3] AG879(20 μM) dramatically decreases proliferation with a variable increase in apoptosis in Cell lines from human leiomyosarcoma (HTB-114, HTB-115, HTB-88), rhabdomyosarcoma (HTB-82, TE-671), prostatic adenocarcinoma (PC-3), acute promyelocytic leukemia (HL-60) and histiocytic lymphoma (U-937). [4] |
体内活性 | AG879(2 mg) induces a decrease in cancer growth in athymic NOD/SCID mice grafted with HTB-114 or HL-60. [4] AG 879(20 mg/kg) treatment keeps 50% of mice absolutely free of RAS-induced sarcomas, and dramatically reduces the size of the growing sarcomas in the nude mice carrying v-Ha-RAS transformed NIH 3T3 cells. [5] |
激酶实验 | AZD3759 is tested at a single 1 μM concentration across each of 124 kinases from Millipore kinase panel at an ATP concentration that is within 15 μM of their corresponding apparent Km values. In brief, recombinant kinases are incubated within an appropriate buffer containing peptide substrate and radiolabelled γ-33P-ATP together with presence or absence of required inhibitor concentration. The reaction is initiated by adding ATP/Mg2+ mix. After incubation for 40 minutes at room temperature, the reaction is stopped by adding 3% phosphoric acid solution. A portion of reaction mix is spotted onto P30 filter mat to trap peptide and washed three times for 5 minutes with phosphoric acid to remove non-specific γ-33P-ATP. The phosphorylated substrate is then measured by scintillation counting, which determined the level of kinase activity inhibition compared to control reactions[1]. |
细胞实验 | Cells are grown in 96-well plates containing 100 μL medium per well. Ten microliters of MTT solution (5 mg/ml in PBS) is added to each well and incubation continued for 4 h at 37 °C. Subsequently, 100 μL 10% SDS in 0.01 M HCl is added. After incubation at 37°C overnight, absorption is measured at 550 nm in an ELISA reader using a reference filter of 690 nm.(Only for Reference) |
别名 | AG 879 |
分子量 | 316.46 |
分子式 | C18H24N2OS |
CAS No. | 148741-30-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 31.7 mg/mL (100 mM)
Ethanol: 7.9 mg/mL (25 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 3.16 mL | 15.7998 mL | 31.5996 mL | 78.9989 mL |
5 mM | 0.632 mL | 3.16 mL | 6.3199 mL | 15.7998 mL | |
10 mM | 0.316 mL | 1.58 mL | 3.16 mL | 7.8999 mL | |
20 mM | 0.158 mL | 0.79 mL | 1.58 mL | 3.9499 mL | |
DMSO | 50 mM | 0.0632 mL | 0.316 mL | 0.632 mL | 1.58 mL |
100 mM | 0.0316 mL | 0.158 mL | 0.316 mL | 0.79 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Tyrphostin AG 879 148741-30-4 Angiogenesis Apoptosis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR Trk receptor HER PDGFR tyrosine phosphorylation antiproliferation ErbB2 Trk Receptor ErbB-1 AG 879 TrKA AG879 Antitumor Tropomyosin related kinase receptor Inhibitor Tyrphostin AG879 p75 Epidermal growth factor receptor Tyrphostin AG-879 HER1 inhibit AG-879 inhibitor