Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Afatinib (BIBW 2992) 是一种不可逆的 EGFR 家族抑制剂,抑制 EGFRwt、EGFRL858R、EGFRL858R/T790M 和 HER2的 IC50分别为0.5 nM、0.4 nM、10 nM 和 14 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 163 | 现货 | ||
2 mg | ¥ 227 | 现货 | ||
5 mg | ¥ 359 | 现货 | ||
10 mg | ¥ 537 | 现货 | ||
25 mg | ¥ 981 | 现货 | ||
50 mg | ¥ 1,490 | 现货 | ||
100 mg | ¥ 1,910 | 现货 | ||
200 mg | ¥ 2,630 | 现货 | ||
500 mg | ¥ 4,120 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 472 | 现货 |
产品描述 | Afatinib (BIBW 2992) is an irreversible inhibitor of EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R/T790M and HER2 with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM , respectively). |
靶点活性 | EGFR:0.5 nM, EGFR (L858R/T790M):10 nM, EGFR (L858R):0.4 nM, HER2:14 nM |
体外活性 | ESCC cell lines were sensitive to afatinib with IC50 concentrations at lower micro-molar range (at 72 hour incubation: HKESC-1 = 0.002 μM, HKESC-2 = 0.002 μM, KYSE510 = 1.090 μM, SLMT-1 = 1.161 μM and EC-1 = 0.109 μM) with a maximum growth inhibition over 95%.?Afatinib can strongly induce G0/G1 cell cycle arrest in HKESC-2 and EC-1 in a dose- and time-dependent manner.?The phosphorylation of ErbB family downstream effectors such as pAKT, pS6 and pMAPK were significantly inhibited in HKESC-2 and EC-1.?Apoptosis was observed in both cell lines at 24 hours after exposure to afatinib, as determined by the presence of cleaved PARP[1]. |
体内活性 | Afatinib could effectively inhibit HKESC-2 tumor growth in mice without obvious toxicity[1]. |
别名 | 阿法替尼, Afatinib free base, BIBW 2992 |
分子量 | 485.94 |
分子式 | C24H25ClFN5O3 |
CAS No. | 850140-72-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 95 mg/mL (195.4 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0579 mL | 10.2893 mL | 20.5787 mL | 51.4467 mL |
5 mM | 0.4116 mL | 2.0579 mL | 4.1157 mL | 10.2893 mL | |
10 mM | 0.2058 mL | 1.0289 mL | 2.0579 mL | 5.1447 mL | |
20 mM | 0.1029 mL | 0.5145 mL | 1.0289 mL | 2.5723 mL | |
50 mM | 0.0412 mL | 0.2058 mL | 0.4116 mL | 1.0289 mL | |
100 mM | 0.0206 mL | 0.1029 mL | 0.2058 mL | 0.5145 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。
Afatinib 850140-72-6 Angiogenesis Autophagy JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR 阿法替尼 NIH-3T3 cells ESCC NSCLC NCI-H1975 inhibit ErbB-1 HKESC-2 EC-1 PKB H1666 c-Met/HGFR Afatinib free base Apoptosis SLMT-1 H3255 BIBW 2992 A431 BIBW-2992 lung cancer Akt Inhibitor BIBW2992 HER2 Epidermal growth factor receptor HKESC-1 anticancer Protein kinase B orally active p38 MAPK HER1 inhibitor