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451492-95-8

中文名稱 AV-412
英文名稱 MP-412
CAS 451492-95-8
分子式 C27H28ClFN6O
分子量 507
MOL 文件 451492-95-8.mol
451492-95-8 結(jié)構(gòu)式 451492-95-8 結(jié)構(gòu)式

基本信息

中文別名
EGFR抑制劑(AV-412)
EGFR抑制劑(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
英文別名
MP-412
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
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

沸點672.9±55.0 °C(Predicted)
密度1.33
儲存條件-20°C儲存
溶解度DMSO: ≥ 50 mg/mL (98.62 mM)
酸度系數(shù)(pKa)11.61±0.43(Predicted)
形態(tài)粉末
顏色White to yellow
AV-412價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-10346AAV-412
AV-412 free base
451492-95-85mg1080元
2024/11/08HY-10346AAV-412
AV-412 free base
451492-95-810mM * 1mLin DMSO1200元
2024/11/08HY-10346AAV-412
AV-412 free base
451492-95-810mg1800元

常見問題列表

生物活性
AV-412 free base (MP-412 free base) 是 EGFR 抑制劑,抑制EGFR,EGFRL858R,EGFRT790M,EGFRL858R/T790M 和 ErbB2的 IC50 值分別為0.75,0.5,0.79,2.3,19 nM。
靶點

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 )

體外研究

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.

體內(nèi)研究

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.

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