|(R,E)-11,26,7-三甲基-56-((4-甲基哌嗪-1-基)甲基)-52,53-二氢-11H,51H-11-氧杂-4-氮杂-5(2,1)-苯并[d]咪唑-2(2,4)-吡啶-1(4,5)-吡唑环十二烷-3-酮|CsnPharm

CAS No.: 2664214-60-0

(R,E)-11,26,7-Trimethyl-56-((4-methylpiperazin-1-yl)methyl)-52,53-dihydro-11H,51H-11-oxa-4-aza-5(2,1)-benzo[d]imidazola-2(2,4)-pyridina-1(4,5)-pyrazolacycloundecaphan-3-one Catalog No. CSN25556

Synonyms: BI-4020

BI-4020 is a noncovalent, new-generation, wild-type EGFR sparing, macrocyclic tyrosine kinase inhibitor.

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生物活性

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 EGFR^{del19 T790M C797S} variant with an IC50 value of 0.2nM in BaF3 cells. BI-4020 also inhibits the double mutant EGFR^{del19 T790M} and primary mutant EGFR^del19. The IC50 values of BI-4020 for BaF3 (EGFR^del19) and BaF3 (EGFR^wt) cells lines are 1nM and 190nM, respectively. Single oral administration of mice bearing subcutaneous PC-9^{del19 T790M C797S} xenotransplants with 10mg/kg BI-4020 suppressed EGFR^{del19 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].
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8427 mL
- 9.2136 mL
- 18.4272 mL
- 5 mM
- 0.3685 mL
- 1.8427 mL
- 3.6854 mL
- 10 mM
- 0.1843 mL
- 0.9214 mL
- 1.8427 mL

技术信息

CAS号

2664214-60-0

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H38N8O2

运输

蓝冰

分子量

542.68

别名

BI-4020

溶解度

DMSO	15.0 mg/mL (27.6 mM)
Ethanol	30.0 mg/mL (55.3 mM)

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(R,E)-11,26,7-Trimethyl-56-((4-methylpiperazin-1-yl)methyl)-52,53-dihydro-11H,51H-11-oxa-4-aza-5(2,1)-benzo[d]imidazola-2(2,4)-pyridina-1(4,5)-pyrazolacycloundecaphan-3-one Catalog No. CSN25556

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