产品
编 号：F478970
分子式：C32H33ClFN5O11
分子量：718.08
分子式：C32H33ClFN5O11
分子量：718.08
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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50mg
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结构图
CAS No: 850140-73-7
产品详情
生物活性：
Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.
体内研究：
Afatinib dimaleate (0 -20 mg/kg，口服，每日一次，持续 25 天) 显示显著的肿瘤消退和 EGFR、HER2、HER3 和 AKT 磷酸化下调。Afatinib dimaleate (15 mg/kg，口服，5 天加停 2 天，持续两周) 强烈抑制 HKESC-2 肿瘤的生长。Animal Model:Athymic NMRI-nu/nu female mice (21–31 g, five to six-week-old, transgenic murine lung cancer model and xenograft models)
Dosage:15 mg/kg, 20 mg/kg
Administration:Orally, daily for 25 days
Result:Resulted in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2% in a standard xenograft model of the epidermoid carcinoma cell line A431, and downregulation of EGFR and AKT phosphorylation. Induced regression of large tumors in this HER2-driven model, effectively controlled xenograft tumor formation by the NCIH1975 cell line, expressing EGFR L858R/T790M, with a T/C value of 12% for doses of 20 mg/kg. Induced more than 50% percent tumor reduction after a 4-week treatment period. Downregulated EGFR, HER2 and HER3 phosphorylation.
Animal Model:Six weeks old female athymic nude mice (nu/nu) (16-20 g)
Dosage:15 mg/kg
Administration:Oral gavage in a schedule of 5 days on plus 2 days off, for two weeks
Result:Strongly inhibited the growth of HKESC-2 tumor. Average tumor sizes of vehicle and treatment at end point are 348 ± 24 mm3 and 108 ± 36 mm3 respectively.
体外研究：
Afatinib dimaleate (100 nM) 充分防止调蛋白刺激的 HER3 磷酸化。 Afatinib dimaleate (0-10000 nM) 有效抑制异位表达 EGFR 的 NIH-3T3 细胞的贴壁非依赖性增殖突变体，并抑制 H1666、H3255 和 NCI 1975 细胞的细胞增殖。 Afatinib dimaleate (48-72 h) 在 HKESC-1、HKESC-2、SLMT-1 和 EC-1 细胞。 Afatinib dimaleate (0-1 μM，24-48 h) 抑制 AKT 和 MAPK 通路，并抑制 ESCC 中的 EGFR 和 AKT 磷酸化cell lines。 Afatinib dimaleate (0-1 μM，16-48 h) 在 HKESC-2 和 EC-1 中诱导 G0/G1 细胞周期停滞。 Afatinib dimaleate (0-1 μM，24-48 h) 有效诱导 HKESC-2 和 EC-1 细胞凋亡。
Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.
体内研究：
Afatinib dimaleate (0 -20 mg/kg，口服，每日一次，持续 25 天) 显示显著的肿瘤消退和 EGFR、HER2、HER3 和 AKT 磷酸化下调。Afatinib dimaleate (15 mg/kg，口服，5 天加停 2 天，持续两周) 强烈抑制 HKESC-2 肿瘤的生长。Animal Model:Athymic NMRI-nu/nu female mice (21–31 g, five to six-week-old, transgenic murine lung cancer model and xenograft models)
Dosage:15 mg/kg, 20 mg/kg
Administration:Orally, daily for 25 days
Result:Resulted in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2% in a standard xenograft model of the epidermoid carcinoma cell line A431, and downregulation of EGFR and AKT phosphorylation. Induced regression of large tumors in this HER2-driven model, effectively controlled xenograft tumor formation by the NCIH1975 cell line, expressing EGFR L858R/T790M, with a T/C value of 12% for doses of 20 mg/kg. Induced more than 50% percent tumor reduction after a 4-week treatment period. Downregulated EGFR, HER2 and HER3 phosphorylation.
Animal Model:Six weeks old female athymic nude mice (nu/nu) (16-20 g)
Dosage:15 mg/kg
Administration:Oral gavage in a schedule of 5 days on plus 2 days off, for two weeks
Result:Strongly inhibited the growth of HKESC-2 tumor. Average tumor sizes of vehicle and treatment at end point are 348 ± 24 mm3 and 108 ± 36 mm3 respectively.
体外研究：
Afatinib dimaleate (100 nM) 充分防止调蛋白刺激的 HER3 磷酸化。 Afatinib dimaleate (0-10000 nM) 有效抑制异位表达 EGFR 的 NIH-3T3 细胞的贴壁非依赖性增殖突变体，并抑制 H1666、H3255 和 NCI 1975 细胞的细胞增殖。 Afatinib dimaleate (48-72 h) 在 HKESC-1、HKESC-2、SLMT-1 和 EC-1 细胞。 Afatinib dimaleate (0-1 μM，24-48 h) 抑制 AKT 和 MAPK 通路，并抑制 ESCC 中的 EGFR 和 AKT 磷酸化cell lines。 Afatinib dimaleate (0-1 μM，16-48 h) 在 HKESC-2 和 EC-1 中诱导 G0/G1 细胞周期停滞。 Afatinib dimaleate (0-1 μM，24-48 h) 有效诱导 HKESC-2 和 EC-1 细胞凋亡。
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