ダコミチニブ 化学特性,用途語,生産方法
外観
白色～うすい黄色粉末～結晶
溶解性
DMSOに溶ける。DMSO(2mg/mL)
用途
ダコミチニブ （ PF-00299804 ）は、 非小細胞肺癌(non-small cell lung cancer; NSCLC)の治療薬。
効能
抗悪性腫瘍薬, 受容体チロシンキナーゼ阻害薬
説明
The epidermal growth factor receptors (EGFR), whose members include ErbB1 (HER1), ErbB2 (HER2), ErbB3 (HER3), and ErbB4 (HER4), are receptor tyrosine kinases that are often over-
expressed in cancer. PF-299804 is a second generation pan-
ErbB receptor tyrosine kinase inhibitor (IC
50s = 6, 45.7, and 73.7 nM for ErbB1, ErbB2, and ErbB4, respectively) that irreversibly binds to the ATP site in the catalytic domains of ErbB receptors. At 15 mg/kg, it demonstrates antitumor activity ranging from delay in tumor growth to complete regression in various tumor xenograft models expressing either wild-
type ErbB or mutant ErbB family members that show resistance to first generation ErbB kinase inhibitors.
使用
PF299804 is a potent, irreversible pan-ErbB inhibitor against ErbB1, ErbB2 and ErbB4 with IC50 of 6 nM, 45.7 nM and 73.7 nM, respectively.
定義
ChEBI: A member of the class of quinazolines that is 7-methoxyquinazoline-4,6-diamine in which the amino group at position 4 is substituted by a 3-chloro-4-fluorophenyl group and the amino group at position 6 is substituted by an (E)-4-(piperidin
1-yl)but-2-enoyl group.
ダコミチニブ 上流と下流の製品情報
原材料
準備製品