阿法替尼
CAS号 | 850140-72-6 | 货号 | BCP04467 |
中文名 | 阿法替尼 | ||
英文名 | Afatinib | ||
中文别名 | Gilotrif;Tovok; | ||
英文别名 | Gilotrif;Tovok;BIBW2992;BIBW-2992;BIBW 2992;(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide; | ||
分子式 | C24H25ClFN5O3 | 分子量 | 485.94 |
生物活性 | 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 Lapatinib 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. | ||
上下游产品 | 439081-18-2(阿法替尼) 850140-73-7(阿法替尼双马来酸盐) | ||
信号通路 | Angiogenesis/Protein Tyrosine Kinase Jak/Stat Pathway | ||
靶 点 | EGFR HER2 |
A novel lead compound CM-118: Antitumor activity and new insight into the molecular mechanism and combination therapy strategy in c-Met- and ALK-dependent cancers
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结构式
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