AV-412
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- CAS号:
- 451492-95-8
- 英文名:
- MP-412
- 英文别名:
- MP-412;AV-412;CS-2307;MP-412 free base;AV-412 (free base);AV 412 free base,AV412 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
- 中文名:
- AV-412
- 中文别名:
- 无盐AV-412;EGFR抑制剂(AV-412);EGFR抑制剂(AV-412 FREE BASE);AV 412,EGFR,ERBB2和ABL受体酪氨酸激酶的有效抑制剂;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
- CBNumber:
- CB52500949
- 分子式:
- C27H28ClFN6O
- 分子量:
- 507
- MOL File:
- 451492-95-8.mol
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AV-412化学性质
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沸点:
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672.9±55.0 °C(Predicted)
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密度:
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1.33
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: ≥ 50 mg/mL (98.62 mM)
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酸度系数(pKa):
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11.61±0.43(Predicted)
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形态:
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Powder
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AV-412性质、用途与生产工艺
AV-412 free base (MP-412 free base) 是 EGFR 抑制剂，抑制EGFR，EGFRL858R，EGFRT790M，EGFRL858R/T790M 和 ErbB2的 IC50 值分别为0.75，0.5，0.79，2.3，19 nM。
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EGFR
0.75 nM (IC
50
)
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ErbB2
19 nM (IC
50
)
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EGFR
L858R
0.51 nM (IC
50
)
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EGFR
L858R/T790M
2.3 nM (IC
50
)
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EGFR
T790M
0.79 nM (IC
50
)
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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.
AV-412
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-10346A | AV-412
AV-412 free base | 451492-95-8 | 2mg | 1100元 |
| 2024/01/25 | HY-10346A | AV-412
AV-412 free base | 451492-95-8 | 5mg | 1800元 |
451492-95-8, AV-412 相关搜索:
- 酶
- 细胞生物学试剂
- 信号转导通路激酶抑制剂
- 抑制剂
- C27H28ClFN6O
- AV 412,EGFR,ERBB2和ABL受体酪氨酸激酶的有效抑制剂
- 无盐AV-412
- 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
- EGFR抑制剂(AV-412)
- 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-1-哌嗪基)-1-丁炔-1-基]-6-喹唑啉基]-2-丙烯酰胺
- 451492-95-8
- AV 412 free base,AV412 free base
- MP-412 free base
- N-[4-(3-chloro-4-fluoroanilino)-7-[3-methyl-3-(4-methylpiperazin-1-yl)but-1-ynyl]quinazolin-6-yl]prop-2-enamide
- CS-2307
- AV-412;MP-412;AV 412;MP 412;AV412;MP412
- AV-412 free base (MP-412 free base)
- N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-methyl-3-(4-methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-2-propenamide
- MP-412
- AV-412
- 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-fluorophenyl)amino)-7-(3-methyl-3-(4-methylpiperazin-1-yl)but-1-yn-1-yl)quinazolin-6-yl)acrylamide
- AV-412 (free base)
- 2-PropenaMide, N-[4-[(3-chloro-4-fluorophenyl)aMino]-7-[3-Methyl-3-(4-Methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-