Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BMS-599626 Hydrochloride (AC480 Hydrochloride) 是一种口服生物有效的HER1、HER2和HER4酪氨酸激酶抑制剂(IC50分别为22、32和190 nM),具有潜在的抗肿瘤活性。BMS-599626 Hydrochloride 抑制人表皮生长因子受体HER1, HER2和HER4,从而抑制过表达这些受体的肿瘤细胞的增殖。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 293 | 现货 | ||
5 mg | ¥ 673 | 现货 | ||
10 mg | ¥ 1,060 | 现货 | ||
25 mg | ¥ 1,990 | 现货 | ||
50 mg | ¥ 3,480 | 现货 | ||
100 mg | ¥ 4,960 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 843 | 现货 |
产品描述 | BMS-599626 Hydrochloride (AC480 Hydrochloride) is an orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases (IC50 =22, 32 and 190 nM, respectively) with potential antineoplastic activity. BMS-599626 Hydrochloride inhibits human epidermal growth factor receptors (HER) HER1, HER2 and HER4, thereby inhibiting the proliferation of tumor cells that overexpress these receptors. |
靶点活性 | HER1:22 nM, HER2:32nM, HER4:190 nM |
体外活性 | BMS-599626 Hydrochloride abrogates HER1 and HER2 signaling and inhibited the proliferation of tumor cell lines that are dependent on these receptors, with IC50s in the range of 0.24 to 1 μM.In GEO cells, HER1 phosphorylation is stimulated by treatment with EGF and is inhibited by BMS-599626 Hydrochloride (IC50=0. 75 μM).There is also nearly complete inhibition of EGF-dependent MAPK (0. 8 μM) but only partial inhibition of AKT signaling.The latter likely reflects the activation of AKT by multiple upstream signals.Treatment of N87 cells with BMS-599626 Hydrochloride leads to the inhibition of HER2 (0. 38 μM), which is expressed to a high level because of gene amplification, as well as MAPK and AKT phosphorylation (0.35 μM for both) [1]. |
体内活性 | BMS-599626 Hydrochloride given before and during irradiation improved the radioresponse of HN5 tumors in vivo [2]. |
别名 | AC480 Hydrochloride |
分子量 | 567.01 |
分子式 | C27H28ClFN8O3 |
CAS No. | 873837-23-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 90.0 mg/mL (158.7 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.7636 mL | 8.8182 mL | 17.6364 mL | 44.0909 mL |
5 mM | 0.3527 mL | 1.7636 mL | 3.5273 mL | 8.8182 mL | |
10 mM | 0.1764 mL | 0.8818 mL | 1.7636 mL | 4.4091 mL | |
20 mM | 0.0882 mL | 0.4409 mL | 0.8818 mL | 2.2045 mL | |
50 mM | 0.0353 mL | 0.1764 mL | 0.3527 mL | 0.8818 mL | |
100 mM | 0.0176 mL | 0.0882 mL | 0.1764 mL | 0.4409 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。
BMS-599626 Hydrochloride 873837-23-1 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors HER AC 480 Hydrochloride BMS599626 Hydrochloride AC480 Hydrochloride AC-480 Hydrochloride BMS 599626 Hydrochloride Inhibitor inhibitor inhibit