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My CartCAS：439081-18-2
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：Off-white to yellow Solid
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| CAS | 439081-18-2 |
| Name | Afatinib |
| Molecular Formula | C24H25ClFN5O3 |
| Molecular Weight | 485.94 |
| Solubility | Soluble in DMSO |
| Purity | HPLC≥98% |
| Appearance | Off-white to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 1308068-626-2 |
| MDL | MFCD12407405 |
| SMILES | CN(C)CC=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OC4CCOC4 |
| Target Point | EGFR |
| Passage | Angiogenesis;Protein Tyrosine Kinase/RTK; JAK/STAT Signaling |
| Background | Afatinib irreversibly inhibits EGFR/ErbB. |
| Biological Activity | Afatinib (BIBW2992)，是酪氨酸激酶ErbB家族的不可逆抑制剂，通过结合表皮生长因子受体（EGFR）/表皮生长因子受体2（HER2）的激酶结构域,从而下调ErbB信号，其IC50值分别为0.5 nM和14 nM。[1] |
| In Vitro | Afatinib在许多过表达EGFR和表达HER2的细胞系中抑制EGF诱导的EGFR磷酸化和细胞增殖，如A431、NIH-3T3-HER2、NCI-N87和BT-474[1]。 |
| In Vivo | Afatinib也被广泛应用于各种动物模型来研究EGFR/HER2的作用。在异种移植和转基因肺癌模型中，口服Afatinib后可抑制癌细胞的生长和存活，诱导肿瘤衰退[2]。此外，Afatinib是已知的EGFR阻断剂，已获批用于EGFR突变非小细胞肺癌患者的治疗[3]。 |
| Data Literature Source | [1]. Eskens FA，Mom CH，Planting AS，Gietema JA，Amelsberg A，Huisman H，et al. A phase I dose escalation study of BIBW 2992，an irreversible dual inhibitor of epidermal growth factor receptor 1 (EGFR) and 2 (HER2) tyrosine kinase in a 2-week on，2-week off schedule in patients with advanced solid tumours. Br J Cancer 2008，98:80-85. [2]. Li D，Ambrogio L，Shimamura T，Kubo S，Takahashi M，Chirieac LR，et al. BIBW2992，an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene 2008，27:4702-4711. [3]. Engle JA，Kolesar JM. Afatinib: A first-line treatment for selected patients with metastatic non-small-cell lung cancer. Am J Health Syst Pharm 2014，71:1933-1938. |
| Unit | Bottle |
| Specification | 5mg 10mM*1mL in DMSO 10mg 20mg |
Afatinib不可逆地抑制EGFR/ErbB。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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