Allitinib tosylate

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Chemical Structure| 1050500-29-2 同义名 : AST-1306 (TsOH); Allitinib; AST-1306 (tosylate); AST-6; AST-1306 TsOH
CAS号 : 1050500-29-2
货号 : A954947
分子式 : C31H26ClFN4O5S
纯度 : 99%
分子量 : 621.08
MDL号 : MFCD17215204
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(80.51 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • EGFR/ErbB1

    EGFR (T790M/L858R), IC50:12 nM

    EGFR, IC50:0.5 nM

  • HER2/ErbB2

    ErbB2, IC50:3.0 nM

  • ErbB4

    ErbB4, IC50:0.8 nM
描述 AST-1306 p-toluenesulfonic acid is an irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases.
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
A431 cells Proliferation assay 72 h Antiproliferative activity against human A431 cells over-expressing EGFR gene after 72 hrs by SRB assay, IC50=0.2 μM 22227214
A549 cells Proliferation assay 72 h Antiproliferative activity against human A549 cells over-expressing EGFR gene after 72 hrs by SRB assay, IC50=6.8 μM 22227214
NCI-H1975 cells Proliferation assay 72 h Antiproliferative activity against human NCI-H1975 cells over-expressing EGFR mutant gene after 72 hrs by SRB assay, IC50=0.7 μM 22227214
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.61mL

0.32mL

0.16mL

8.05mL

1.61mL

0.81mL

16.10mL

3.22mL

1.61mL
参考文献

[1]Xie H, Lin L, et al. AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo. PLoS One. 2011;6(7):e21487.

[2]Zhang H, Wang YJ, et al. AST1306, a potent EGFR inhibitor, antagonizes ATP-binding cassette subfamily G member 2-mediated multidrug resistance. Cancer Lett. 2014 Aug 1;350(1-2):61-8.