Afatinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

阿法替尼是一种口服生物可利用的苯胺基喹唑啉衍生物，是受体酪氨酸激酶 (RTK) 表皮生长因子受体 (ErbB；EGFR) 家族的抑制剂，具有抗肿瘤活性。

Afatinib is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity. Upon administration, afatinib selectively and irreversibly binds to and inhibits the epidermal growth factor receptors 1 (ErbB1; EGFR), 2 (ErbB2; HER2), and 4 (ErbB4; HER4), and certain EGFR mutants, including those caused by EGFR exon 19 deletion mutations or exon 21 (L858R) mutations. This may result in the inhibition of tumor growth and angiogenesis in tumor cells overexpressing these RTKs. Additionally, afatinib inhibits the EGFR T790M gatekeeper mutation which is resistant to treatment with first-generation EGFR inhibitors. EGFR, HER2 and HER4 are RTKs that belong to the EGFR superfamily; they play major roles in both tumor cell proliferation and tumor vascularization and are overexpressed in many Y cell types.

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BIBW2992

Angiogenesis

EGFR

EGFR (L858R)| EGFR (L858R/T790M)| EGFR (wt)| HER2

Cancer

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439081-18-2

485.94

C24H25ClFN5O3

>98% (HPLC)

Ethanol: 15 mg/mL (30.86 mM); DMSO: 97 mg/mL (199.61 mM)

CN(C)C/C=C/C(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)O[C@H]4CCOC4

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(-20℃)

With Ice Pack

≥ 2 years