AV 412
|
|
|
- CAS号:
- 451493-31-5
- 英文名:
- 2-PropenaMide, N-[4-[(3-chloro-4-fluorophenyl)aMino]-7-[3-Methyl-3-(4-Methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-, 4-Methylbenzenesulfonate (1:2)
- 英文别名:
- MP-412;MP412;AV-412 / MP-412;AV-412 Tosylate;451492-95-8 (AV-412 FREE BASE);MP-412;AV412;AV 412;MP412;MP 412;AV412,EGFR,MP-412,Inhibitor,inhibit,MP 412,HER1,Epidermal growth factor receptor,AV 412,AV-412,ErbB-1;N-[4-(3-Chloro-4-fluoroanilino)-7-[3-methyl-3-(4-methylpiperazin-1-yl)but-1-ynyl]quinazolin-6-yl]prop-2-enamide tosylate;N-[4-(3-chloro-4-fluoroanilino)-7-[3-methyl-3-(4-methylpiperazin-1-yl)but-1-ynyl]quinazolin-6-yl]prop-2-enamide,4-methylbenzenesulfonic acid;N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(3-methyl-3-(4-methylpiperazin-1-yl)but-1-yn-1-yl)quinazolin-6-yl)acrylamide bis(4-methylbenzenesulfonate);N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-methyl-3-(4-methyl-1-piperazinyl)-1-butynyl]-6-quinazolinyl]-2-propenamide bis(4-methylbenzenesulfonate)
- 中文名:
- AV 412
- 中文别名:
- 化合物AV-412;MP-412; MP 412; MP412; AV-412; AV 412; AV412
- CBNumber:
- CB02626693
- 分子式:
- C41H44ClFN6O7S2
- 分子量:
- 851.4054632
- MOL File:
- 451493-31-5.mol
|
|
|
AV 412化学性质
-
储存条件:
-
Store at -20°C
-
|
-
溶解度:
-
DMSO:21.5(Max Conc. mg/mL);25.29(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:3):0.25(Max Conc. mg/mL);0.29(Max Conc. mM)
DMF:15.0(Max Conc. mg/mL);17.64(Max Conc. mM)
Ethanol:0.25(Max Conc. mg/mL);0.29(Max Conc. mM)-
|
-
形态:
-
Powder
-
|
AV 412性质、用途与生产工艺
AV-412 (MP412) 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。
|
EGFR
0.75 nM (IC
50
)
|
EGFR
L858R
0.5 nM (IC
50
)
|
EGFR
T790M
0.79 nM (IC
50
)
|
EGFR
L858R/T790M
2.3 nM (IC
50
)
|
ErbB2
19 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.
AV 412
上下游产品信息
上游原料
下游产品
451493-31-5, AV 412 相关搜索:
- 2C7H8O3SC27H28ClFN6O
- C27H28ClFN6O2C7H8O3S
- MP-412; MP 412; MP412; AV-412; AV 412; AV412
- 化合物AV-412
- 451493-31-5
- N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(3-methyl-3-(4-methylpiperazin-1-yl)but-1-yn-1-yl)quinazolin-6-yl)acrylamide bis(4-methylbenzenesulfonate)
- AV412,EGFR,MP-412,Inhibitor,inhibit,MP 412,HER1,Epidermal growth factor receptor,AV 412,AV-412,ErbB-1
- N-[4-(3-chloro-4-fluoroanilino)-7-[3-methyl-3-(4-methylpiperazin-1-yl)but-1-ynyl]quinazolin-6-yl]prop-2-enamide,4-methylbenzenesulfonic acid
- MP-412;AV412;AV 412;MP412;MP 412
- N-[4-(3-Chloro-4-fluoroanilino)-7-[3-methyl-3-(4-methylpiperazin-1-yl)but-1-ynyl]quinazolin-6-yl]prop-2-enamide tosylate
- 451492-95-8 (AV-412 FREE BASE)
- MP-412;MP412
- AV-412 Tosylate
- N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-methyl-3-(4-methyl-1-piperazinyl)-1-butynyl]-6-quinazolinyl]-2-propenamide bis(4-methylbenzenesulfonate)
- AV-412 / MP-412
- 2-PropenaMide, N-[4-[(3-chloro-4-fluorophenyl)aMino]-7-[3-Methyl-3-(4-Methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-, 4-Methylbenzenesulfonate (1:2)