Afatinib NEW
| Price | $30 | $47 | $78 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-12 |
Product Details
| Product Name: Afatinib | CAS No.: 850140-72-6 |
| Purity: 99.9% | Supply Ability: 10g |
| Release date: 2024/11/12 |
Product Introduction
Bioactivity
| 名稱 | Afatinib |
| 描述 | Afatinib (BIBW 2992) is an irreversible inhibitor of the 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. |
| 體外活性 | METHODS: NSCLC cells NCI-H1975, NCI-H1781, HCC827 and A549 were treated with Afatinib (0.0001-10 μM) for 72 h. Cell viability was measured by MTS assay. RESULTS: Afatinib inhibited the survival of tumor cell lines harboring wild-type (H1666) or L858R/T790M (NCI-H1975) EGFR. Afatinib is also effective against NSCLC cell lines expressing HER2 776insV (NCI-H1781) or EGFR E746_A750del (HCC827), but is inactive against A549 cells expressing wild-type EGFR and HER2 but also harboring the oncogenic Kras G12S point mutation. [1] METHODS: BEAS-2B cells overexpressing wild-type or mutant HER2 were treated with Afatinib (0.1 μM) for 6 h, and target protein expression levels were measured by Western Blot. RESULTS: Afatinib treatment inhibited the phosphorylation of HER2, EGFR and AKT. [2] |
| 體內(nèi)活性 | METHODS: To assay antitumor activity in vivo, Afatinib (20 mg/kg, 1.8% HP-beta-CD + 5% acetic acid (10%) + aqueous Natrosol (0.5%)) was administered by gavage to NMRI-nu/nu mice bearing A431 xenografts once daily for 25 days. RESULTS: Afatinib resulted in significant tumor regression with a cumulative treatment/control tumor volume ratio (T/C ratio) of 2% and downregulation of EGFR and AKT phosphorylation. [1] |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 45 mg/mL (92.6 mM) |
| 關(guān)鍵字 | NIH-3T3 cells | ESCC | NSCLC | NCI-H1975 | Afatinib | inhibit | ErbB-1 | HKESC-2 | EC-1 | PKB | H1666 | c-Met/HGFR | Apoptosis | SLMT-1 | H3255 | A431 | BIBW-2992 | lung cancer | EGFR | Akt | Inhibitor | BIBW2992 | HER2 | Autophagy | Epidermal growth factor receptor | HKESC-1 | anticancer | Protein kinase B | orally active | p38 MAPK | HER1 |
| 相關(guān)產(chǎn)品 | Hydroxychloroquine | Guanidine hydrochloride |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 膜蛋白靶向化合物庫(kù) | 酪氨酸激酶分子庫(kù) | 藥物功能重定位化合物庫(kù) | FDA 上市激酶抑制劑庫(kù) | FDA 上市藥物庫(kù) | 抗癌上市藥物庫(kù) | 抗衰老化合物庫(kù) | 已知活性化合物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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