产品说明书

BI-4020

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Chemical Structure| 2664214-60-0 同义名 : -
CAS号 : 2664214-60-0
货号 : A1228809
分子式 : C30H38N8O2
纯度 : 99%+
分子量 : 542.675
MDL号 : MFCD32263045
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(460.68 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

1M HCl: 100 mg/mL(184.27 mM)，配合低频超声，并调节pH至1
动物实验配方：
生物活性
靶点

  • mutant EGFR

    EGFRdel19 T790M C797S, IC50:0.2 nM
描述 Epidermal growth factor receptor (EGFR) is a receptor tyrosine kinase essential for cell proliferation and differentiation. Mutations in the EGFR gene are observed in non-small cell lung cancer. BI-4020 is a non-covalent, macrocyclic tyrosine kinase inhibitor that inhibits the triple mutant EGFRdel19 T790M C797S variant with an IC50 value of 0.2nM in BaF3 cells. BI-4020 also inhibits the double mutant EGFRdel19 T790M and primary mutant EGFRdel19. The IC50 values of BI-4020 for BaF3 (EGFRdel19) and BaF3 (EGFRwt) cells lines are 1nM and 190nM, respectively. Single oral administration of mice bearing subcutaneous PC-9del19 T790M C797S xenotransplants with 10mg/kg BI-4020 suppressed EGFRdel19 T790M C797S phosphorylation 5- to 10-fold compared with vehicle-treated controls. Daily oral treatment with 10mg/kg BI-4020 for 19 days led to 121% tumor growth inhibition in the same mouse xenograft model[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.84mL

0.37mL

0.18mL

9.21mL

1.84mL

0.92mL

18.43mL

3.69mL

1.84mL
参考文献

[1]Engelhardt H, Böse D, Petronczki M. et al. Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors. J Med Chem. 2019 Nov 27;62(22):10272-10293.