451492-95-8
![451492-95-8 结构式](/CAS/GIF/451492-95-8.gif)
基本信息
EGFR抑制剂(AV-412 FREE BASE)
N-(4-((3-氯-4-氟苯基)氨基)-7-(3-甲基-3-(4-甲基哌嗪-1-基)丁-1-炔-1-基)喹唑啉-6-基)丙烯酰胺
N-[4-[(3-氯-4-氟苯基)氨基]-7-[3-甲基-3-(4-甲基-1-哌嗪基)-1-丁炔-1-基]-6-喹唑啉基]-2-丙烯酰胺
AV-412
CS-2307
MP-412 free base
AV-412 (free base)
AV-412 free base (MP-412 free base)
AV-412
MP-412
AV 412
MP 412
AV412
MP412
N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(3-methyl-3-(4-methylpiperazin-1-yl)but-1-yn-1-yl)quin
N-[4-(3-chloro-4-fluoroanilino)-7-[3-methyl-3-(4-methylpiperazin-1-yl)but-1-ynyl]quinazolin-6-yl]prop-2-enamide
N-(4-((3-chloro-4-fluorophenyl)amino)-7-(3-methyl-3-(4-methylpiperazin-1-yl)but-1-yn-1-yl)quinazolin-6-yl)acrylamide
物理化学性质
报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
2024/04/30 | HY-10346 | AV-412 AV-412 | 451492-95-8 | 5mg | 1080元 |
2024/04/30 | HY-10346A | AV-412 AV-412 free base | 451492-95-8 | 5mg | 1080元 |
2024/04/30 | HY-10346A | AV-412 AV-412 free base | 451492-95-8 | 10mM * 1mLin DMSO | 1200元 |
常见问题列表
EGFR 0.75 nM (IC 50 ) |
ErbB2 19 nM (IC 50 ) |
EGFR L858R 0.51 nM (IC 50 ) |
EGFR L858R/T790M 2.3 nM (IC 50 ) |
EGFR T790M 0.79 nM (IC 50 ) |
AV-412 inhibits autophosphorylation of EGFR and ErbB2 with IC 50 of 43 and 282 nM, respectively. AV-412 also inhibits epidermal growth factor (EGF)-dependent cell proliferation with an IC 50 of 100 nM. AV-412 abrogates EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR.
In animal studies using cancer xenograft models, AV-412 (30 mg/kg) demonstrates complete inhibition of tumor growth of the A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively. AV-412 suppresses autophosphorylation of EGFR and ErbB2 at the dose corresponding to its antitumor efficacy. When various dosing schedules are applied, AV-412 shows significant effects with daily and every-other-day schedules, but not with a once-weekly schedule, suggesting that frequent dosing is preferable for this compound. Furthermore, AV-412 shows a significant antitumor effect on the ErbB2-overexpressing breast cancer KPL-4 cell line, which is resistant to gefitinib.