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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-TQB3804
TQB3804

Chemical Structure : TQB3804

CAS No.: 2267329-76-8

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TQB3804 (TQB-3804, EGFR-IN-7)

货号: PC-38032Not For Human Use, Lab Use Only.

TQB3804 (EGFR-IN-7) is a selective, potent, 3rd generation EGFR C797S inhibitor with IC50 of 1.07 nM and 0.13 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TQB3804 (EGFR-IN-7) is a selective, potent, 3rd generation EGFR C797S inhibitor with IC50 of 1.07 nM and 0.13 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively.
TQB3804 displays potent enzymatic activities for EGFRd746-750/T790M/C797S, EGFRL858R/T790M/C797S, EGFRd746-750/T790M, and EGFRL858R/T790M with IC50 of 0.46, 0.13, 0.26, and 0.19 nM respectively, and has similar enzymatic activity for EGFRWT (IC50=1.07 nM) to Osimertinib.
TQB3804 shows expected anti-proliferative activity Ba/F3 (EGFRd746-750/T790M/C797S), NCI-H1975 (EGFRd746-750/T790M/C797S), PC9 (EGFRd746-750), and A431 (EGFRWT), with IC50 of 26.8, 163, 45, and 147 nM, respectively.
TQB3804 inhibits phosphorylation for EGFR in Ba/F3 (EGFRd746-750/T790M/C797S) cell line with IC50 of 18.5 nM.
TQB3804 significantly inhibits tumor growth in the triple mutant Ba/F3 (EGFRd746-750/T790M/C797S), NCI-H1975 (EGFRd746-750/T790M/C797S), and PC9 (EGFRd746-750/T790M/C797S) CDX models.

物理化学性质&存储条件

分子量 694.62
分子式 C32H41BrN9O2P
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2,4-Pyrimidinediamine, 5-bromo-N4-[5-(dimethylphosphinyl)-6-quinoxalinyl]-N2-[2-methoxy-5-methyl-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-

参考文献

1. Rui-Fang Dong, et al. Pharmacol Res. 2021 May:167:105583.

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