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| 品牌 | absin | CAS | 439081-18-2 |
|---|---|---|---|
| 分子式 | C24H25ClFN5O3 | 纯度 | ＞98% |
| 分子量 | 485.94 | 货号 | abs810678 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | irreversibly inhibits EGFR/HER2 includin | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Afatinib 439081-18-2
| 产品描述 | |
| 描述 | BIBW2992 (Afatinib, Tomtovok, Tovok) irreversibly inhibits EGFR/HER2 including EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively. |
| 纯度 | >98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | 阿法替尼;(E/Z)-Afatinib |
| 外观 | White to off-white powder |
| 可溶性/溶解性 | DMSO ：97 mg/mL (199.61 mM) Ethanol ：15 mg/mL (30.86 mM) |
| 生物活性 | |
| 靶点 | EGFR (L858R)；EGFR (wt)；ErbB4；EGFR (L858R/T790M)；HER2 |
| In vitro(体外研究) | BIBW2992 shows potent activity against both wild-type and mutant forms of EGFR and HER2. It is similar to Gefitinib in potency against L858R EGFR, but about 100-fold more active against the Gefitinib resistant L858R-T790M EGFR double mutant. BIBW2992 exhibits potent effects on both EGFR and HER2 phosphorylation in vivo. It compares favorably to reference compounds (such as Lapatnib et al.) in all cell types tested, such as human epidermoid carcinoma cell line A431 expressing wt EGFR, murine NIH-3T3 cells transfected with wt HER2, as well as breast cancer cell line BT-474 and gastric cancer cell line NCI-N87, which express endogenous HER2. |
| In vivo(体内研究) | Daily oral administration of BIBW2992 at 20 mg/kg for 25 days results in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2%. Reduced phosphorylation of EGFR and AKT is confirmed by immunohistochemical staining of tissue sections. Therefore, like laptinib and neratinib, BIBW2992 is a next generation tyrosine kinase inhibitor (TKI) that inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases irreversibly. BIBW2992 is not only active against EGFR mutations targeted by first generation TKIs like Erlotinib or Gefitinib, but also against those insensitive to these standard therapies. |
| 研究领域 | |
| 研究领域 | CancerGrowth factorsEGF CancerOncoproteins/suppressorsOncoproteinsGrowth factor receptors CancerSignal transductionProtein phosphorylationTyrosine kinasesReceptor tyrosine kinases CancerTumor biomarkersReceptors Cell CycleCell differentiation MicrobiologyOrganismVirusDNA VirusssRNA positive strand virusSARS Coronavirus NeuroscienceDevelopment NeuroscienceProcesses Signal TransductionGrowth Factors/HormonesEGF Signal TransductionProtein PhosphorylationTyrosine KinasesReceptor Tyrosine Kinases Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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