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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
4°C, sealed storage, away from moisture
- 英文名：
Abivertinib maleate; AC0010 maleate
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1557268-88-8
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥930.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥280.0 |
| 规格： | 5 mg | 产品价格： | ￥700.0 |
| 规格： | 10 mg | 产品价格： | ￥1200.0 |
| 规格： | 25 mg | 产品价格： | ￥2200.0 |
| 规格： | 50 mg | 产品价格： | ￥3500.0 |
| 规格： | 100 mg | 产品价格： | ￥5500.0 |
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Avitinib maleate
CAS No. : 1557268-88-8
MCE 国际站：Avitinib maleate
产品活性：Avitinib (Abivertinib) maleate 是第三代、不可逆、具有口服活性的选择性 EGFR 抑制剂，针对 EGFR L858R、EGFR T790M 和野生型 EGFR 的 IC50 值为 0.18 nM、0.18 nM、7.68 nM。Avitinib maleate 也是一种 BTK 抑制剂，可诱导套细胞淋巴瘤细胞凋亡 (apoptosis) 并抑制 BTK 磷酸化。Avitinib maleate 显示出抗癌作用。
研究领域：JAK/STAT Signaling | Protein Tyrosine Kinase/RTK | Apoptosis
In Vitro: Avitinib (AC0010; 0.13 nM-2 μM; 2 h) maleate selectively inhibits mutant EGFR phosphorylation with IC50 values of 7.3 and 2.8 nM in NCI-H1975 and NIH/3T3_TC32T8 cells, about 115- and 298-fold more sensitive than that of the inhibition of wild-type EGFR in A431. Avitinib potently inhibits EGFR-Tyr1068 phosphorylation in NCI-H1975 cells, and the selectivity ratio is at 65-fold for NCI-H1975 cells versus A431 cells. In addition to inhibition of EGFR-Tyr1068 phosphorylation, Avitinib inhibits phosphorylation of the downstream targets Akt and ERK1/2 in NCI-H1975 and HCC827 cells.
In Vivo: Avitinib (AC0010; 12.5-500 mg/kg; orally administration; once daily; for 14 days) maleate inhibits EGFR-mutant tumor growth but not wild-type EGFR tumor growth in xenograft models over extended duration.
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文献和实验sodium maleate pH 5.2 (3 x 5'). 8). en bloc stain in 1% uranyl acetate in maleate buffer pH 5.2 (1 hr RT). Using uranyl acetate at low pH will improve membrane contrast. Analternative contrasting method, which adds even more membrane contrast
糖液500ml稀释后缓慢滴入。 马来酸麦角新碱（ergometrine maleate）口服，0.2～0.5mg/次。肌内注射，0.2～0.5mg/次，必要时半小时后重复一次。静脉滴注0.2mg以5%葡萄糖溶液稀释后应用。极量：肌内或静脉注射，0.5mg/次，1mg/日。 酒石酸麦角胺（ergotamine tartrate）口服1mg/次。皮下或肌内注射，0.25mg/次。 麦角胺咖啡因片 每片含酒石酸麦角胺1mg，咖啡因100mg。偏头痛发作时即口服半片至1片半；如无效，可于
滴注5～10U/次，可用5%葡萄糖液500ml稀释后缓慢滴入。 马来酸麦角新碱（ergometrine maleate）口服，0.2～0.5mg/次。肌内注射，0.2～0.5mg/次，必要时半小时后重复一次。静脉滴注0.2mg以5%葡萄糖溶液稀释后应用。极量：肌内或静脉注射，0.5mg/次，1mg/日。 酒石酸麦角胺（ergotamine tartrate）口服1mg/次。皮下或肌内注射，0.25mg/次。 麦角胺咖啡因片 每片含酒石酸麦角胺1mg，咖啡因100mg。偏头痛发作
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