Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Sapitinib (AZD-8931) 是可逆的 ATP 竞争型 EGFR 抑制剂,对 EGFR、ErbB2 和 ErbB3的IC50值分别为4、3 和 4 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 198 | 现货 | ||
2 mg | ¥ 319 | 现货 | ||
5 mg | ¥ 577 | 现货 | ||
10 mg | ¥ 995 | 现货 | ||
25 mg | ¥ 1,660 | 现货 | ||
50 mg | ¥ 2,470 | 现货 | ||
100 mg | ¥ 3,680 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 686 | 现货 |
产品描述 | Sapitinib (AZD-8931) , a reversible, ATP competitive inhibitor of EGFR(IC50=4 nM), ErbB2(IC50=3 nM) and ErbB3(IC50=4 nM), is more effective over Gefitinib or Lapatinib against NSCLC cell, 100-fold more specific for the ErbB family over MNK1 and Flt. |
靶点活性 | EGFR:4 nM, ErbB2:3 nM, ERB3:4 nM |
体外活性 | AZD8931 shows different potency to NSCLC and SCCHN cell lines. AZD8931 has high sensitivity to PC-9 cells (EGFR activating mutation) with GI50 of 0.1 nM and low activity to NCI-1437 cells with GI50 above 10 μM. AZD8931 exhibits more potency against phospho-EGFR, phospho-erbB2 and phospho-erbB3 than either lapatinib or gefitinib in PE/CA-PJ41, PE/CA-PJ49, DOK and FaDu cells. [1] |
体内活性 | AZD8931 reveals antitumor activity in BT474c, Calu-3, LoVo, FaDu and PC-9 xenografts. AZD8931 could reduce p-Akt, Ki67 expression and p-ERK in BT474c xenografts following acute treatment. AZD8931 also causes induction of the M30 apoptosis marker. Furthermore, AZD8931 shows greater proapoptotic effect compared with gefitinib and lapatinib in LoVo xenografts. [1] |
激酶实验 | Isolated kinase assays: The intracellular kinase domains of human EGFR and erbB2 are cloned and expressed in the baculovirus/Sf21 system. The inhibitory activity of AZD8931 is determined with ATP at Km concentrations (0.4 mM for erbB2 and 2 mM for EGFR) using the ELISA method. |
细胞实验 | To determine the antiproliferative activity against cell lines grown in vitro, AZD8931 is tested in a panel of NSCLC and SCCHN cell lines. Cells are incubated for 96 hours with AZD8931 (0.001-10 μM). Viable cell number is determined by 4 hours of incubation with MTS Colorimetric Assay reagent and absorbance measured at 490 nm on a spectrophotometer. (Only for Reference) |
别名 | 沙普替尼, AZD-8931 |
分子量 | 473.93 |
分子式 | C23H25ClFN5O3 |
CAS No. | 848942-61-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 38 mg/mL (80.2 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.11 mL | 10.5501 mL | 21.1002 mL | 52.7504 mL |
5 mM | 0.422 mL | 2.11 mL | 4.22 mL | 10.5501 mL | |
10 mM | 0.211 mL | 1.055 mL | 2.11 mL | 5.275 mL | |
20 mM | 0.1055 mL | 0.5275 mL | 1.055 mL | 2.6375 mL | |
50 mM | 0.0422 mL | 0.211 mL | 0.422 mL | 1.055 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。
Sapitinib 848942-61-0 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR inhibit Inhibitor HER1 ErbB-1 AZD8931 Epidermal growth factor receptor 沙普替尼 AZD 8931 AZD-8931 inhibitor